Journal articles: 'Biological active compounds'

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Novruzov, E. N. "Biologically Active Compounds and Biological Activity of Physalis alkekengi (Solanaceae)." Растительные ресурсы 56, no. 3 (2020): 280–88. http://dx.doi.org/10.31857/s0033994620020077.

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Savchuk, Ya I., K. S. Tsyhanenko, O. V. Andrienko, and I. M. Kurchenko. "The New Biologically Active Metabolites from Aspergillus niveus 2411." Mikrobiolohichnyi Zhurnal 83, no. 4 (August 17, 2021): 74–85. http://dx.doi.org/10.15407/microbiolj83.04.074.

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Pharmacological science possesses a significant number of compounds with antibiotic activity. By now the chemical structures have been identified and their properties have been described for the great number; many of them found practical use. But the main stimulus for the further new antibiotic compounds search is the acquired resistance of pathogenic organisms. Our previous investigations were devoted to antibiotic activity of Aspergillus niveus that is known as a producer of ferment preparations with wide activity spectrum. Aim. This investigation became the follow-up of our previous studies and its main task was to isolate, purify and obtain biologically active metabolite(s) from A. niveus 2411 strain in crystalline form, and to study its (their) physicochemical properties and biological activity. Methods. Biologically active metabolites were obtained by extraction, two-step column chromatography and recrystallization methods. The obtained substances were characterized by physical-chemical and microbiological methods. Results. Two substances in crystalline form with different spectrum of antibiotic activity against indicator test-cultures were obtained. The substance AN4 showed antibacterial, antifungal, and phytotoxic activities, while AN7 showed only antibacterial activity. Neither of obtained compounds showed dermatocidal or toxigenic activity in rabbit skin test. Obtained spectral characteristics of substances suggest that AN4 and AN7 substances are similar and belong to compounds with cyclic structures, have double linkage, methyl, aromatic, and carboxyl groups. Conclusions. Obtained data showed that antibiotic activity of A. niveus 2411 depend on the complex of biologically active metabolites with different biological and physicochemical properties. Two compounds AN4 and AN7 were isolated and purified from the fungal cultural filtrate of A. niveus 2411. The data of IR and UV spectra of these compounds and their profiles of biological activity don’t have significant differences with those of citrinin – a metabolite of A. niveus with antibiotic properties. However, based on the results obtained and comparisons with the data of other authors on metabolites of A. niveus, we suggest that the substances we isolated may be derivatives of citrinin.

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Poljakovic, Melita, Majda Srabovic, and Ekrem Pehlic. "Synthesis and Morphology of Biological Active Compounds." Journal of Scientific Research and Reports 3, no. 19 (January 10, 2014): 2562–73. http://dx.doi.org/10.9734/jsrr/2014/12033.

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Dang, Nga Phuong, Bjarne Landfald, and Nils Peder Willassen. "Biological surface-active compounds from marine bacteria." Environmental Technology 37, no. 9 (November 2, 2015): 1151–58. http://dx.doi.org/10.1080/09593330.2015.1103784.

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Ježek, Jan, Milan Zaoral, Miloš Buděšínský, Jiří Günther, and Jiří Rotta. "Muramyl-dipeptide analogues: Synthesis and biological activities." Collection of Czechoslovak Chemical Communications 53, no. 11 (1988): 2897–906. http://dx.doi.org/10.1135/cccc19882897.

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In the search for immunoadjuvant active compounds without pyrogenic activity we prepared N-Ac-norMur-L-Abu-D-Gln-O-Bu (V), N-Ac-Mur-L-Abu-D-Gln-O-Bu (VII) and their respective α-benzylglycosides VI and VIII. All the prepared compounds are nonpyrogenic. In the delayed hypersensitivity test, compound V is inactive, VI is comparable to MDP, VII is more and VIII is less active than MDP.

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Plackal George, Blassan, Parimelazhagan Thangaraj, Cheruthazhakkatt Sulaiman, Shanmughavel Piramanayagam, and Sathish Kumar Ramaswamy. "Bioassay Directed Isolation and Biological Evaluation of Compounds Isolated fromRubus fairholmianusGard." BioMed Research International 2014 (2014): 1–15. http://dx.doi.org/10.1155/2014/204340.

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Thein vitroandin silicoanalysis ofRubus fairholmianusacetone extract for antioxidant, antiproliferative, and anti-inflammatory activity led to the isolation of six compounds. Amongst all the six isolated compounds tested, 1-(2-hydroxyphenyl)-4-methylpentan-1-one (compound1) and 2-[(3-methylbutoxy) carbonyl] benzoic acid (compound2) were found to be more active in inhibiting BRCA and COX target proteins, which also showed the better results for DPPH and ABTS radical scavenging assays. The promising results of this investigation emphasize the importance of usingR. fairholmianusin the treatment of radical generated disorders mainly cancer and other inflammatory diseases.

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Appell, Kenneth C., Thomas D. Y. Chung, Michael J. H. Ohlmeyer, Nolan H. Sigal, John J. Baldwin, and Daniel Chelsky. "Biological Screening of a Large Combinatorial Library." Journal of Biomolecular Screening 1, no. 1 (February 1996): 27–31. http://dx.doi.org/10.1177/108705719600100111.

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Encoding technology has allowed for the creation of libraries of 50,000 or more low-molecular-weight compounds for biological testing. The current challenge is to properly and efficiently screen among these compounds for useful biological activities. In this example, actives against two related G-protein coupled receptors were sought from a combinatorial library of 56,000 members. The library was synthesized on solid phase using the split synthesis method and photochemically released for testing. At a screening concentration of 0.5-1 /LM, 86 unique structures were identified as active against one receptor and 24 were active against the other. Due to the random nature of compound sampling, five library equivalents or 280,000 beads were screened to ensure greater than 99% representation of library members. As a result, many actives appeared multiple times in the screen, verifying the encoding process. Further confirmation was obtained by resynthesis and testing of predicted active structures. A clear bias for specific "R" groups at each point of variation in the combinatorial library with little overlap between the two receptors has produced a clear structure-activity relationship on which to base further work.

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Asakawa, Yoshinori. "Biologically active compounds from bryophytes." Pure and Applied Chemistry 79, no. 4 (January 1, 2007): 557–80. http://dx.doi.org/10.1351/pac200779040557.

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Liverworts produce a great variety of lipophilic terpenoids, aromatic compounds, and acetogenins. Many of these constituents have characteristic scents, pungency, and bitterness, and display a quite extraordinary array of bioactivities and medicinal properties. These expressions of biological activity are summarized and discussed, and examples are given of the potential of certain lead compounds for structure-activity studies and synthesis.

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Khan, Khalid M., Zafar S. Saifyb, Abdullah Khan, Mansoor Ahmed, Muhammed Saeed, Raid J. Abdel-Jalil, Gerald Griibler, and Wolfgang Voelter. "Syntheses of Selected Quaternary Phenacylbromopyridinium Compounds and their Biological Evaluation." Zeitschrift für Naturforschung B 54, no. 9 (September 1, 1999): 1210–18. http://dx.doi.org/10.1515/znb-1999-0920.

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The studies, presented here, deal with the synthetic modification of 5-bromonicotinic acid on its nitrogen nucleus. The synthetic transformations were carried out by reacting equimolar amounts of 5-bromonicotinic acid and phenacyl halides in acetone. A range of phenacyl halides were used with the objective of getting a variety of quaternary ammonium salts of 5- bromonicotinic acid derivatives as multipurpose biologically active compounds. Twelve quaternary ammonium salts of 5-bromonicotinic acid have been synthesized and tested for cytotoxicity, antibacterial and antifungal activities. These compounds showed promising cytotoxicity against Artemia salina. Two compounds, 3-carboxy-1-(4′-methylphenacyl)-5-bromopyridinium bromide (2) and 3-carboxy-1-(4′-nitrophenacyl)-5-bromopyridinium bromide (12), were highly active against Gram-positive and Gram-negative bacteria among all the tested compounds. All the compounds were examined for antifungal activity against fifteen fungal cultures, but none of these compounds proved to be effective against these fungi. The parent compounds and its derivatives were also examined for their effect on mean arterial blood pressure in anaesthetized rats. Compounds 7 and 8 were found to be twofold more active than the parent compound. The rest of the products showed blood pressure lowering effects comparable to the parent compound. All compounds were characterised via elemental analysis UV, IR , mass and 1H NMR spectroscopy.

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10

Mourad, mohamed. "BIOLOGICAL STUDIES ON ACTIVE COMPOUNDS FROM TRICHODERMA VIRIDE." Al-Azhar Journal of Pharmaceutical Sciences 53, no. 1 (March 1, 2016): 143–59. http://dx.doi.org/10.21608/ajps.2016.6895.

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11

Gorecki, P., and A. Mścisz. "Semisynthetic Transformations of Fraxin to Biological Active Compounds." Planta Medica 54, no. 06 (December 1988): 577. http://dx.doi.org/10.1055/s-2006-962587.

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12

Ziarani, Ghodsi M., Fatemeh Mohajer, Razieh Moradi, and Parisa Mofatehnia. "The Molecular Diversity Scope of Urazole in the Synthesis of Organic Compounds." Current Organic Synthesis 16, no. 7 (December 26, 2019): 953–67. http://dx.doi.org/10.2174/1570179416666190925162215.

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Background: As a matter of fact, nitrogen as a hetero atom among other atoms has had an important role in active biological compounds. Since heterocyclic molecules with nitrogen are highly demanded due to biological properties, 4-phenylurazole as a compound containing nitrogen might be important in the multicomponent reaction used in agrochemicals, and pharmaceuticals. Considering the case of fused derivatives “pyrazolourazoles” which are highly applicable because of their application for analgesic, antibacterial, anti-inflammatory and antidiabetic activities as HSP-72 induction inhibitors (I and III) and novel microtubule assembly inhibitors. It should be mentioned that spiro-pyrazole also has biological activities like cytotoxic, antimicrobial, anticonvulsant, antifungal, anticancer, anti-inflammatory, and cardiotonic activities. Objective: Urazole has been used in many heterocyclic compounds which are valuable in organic syntheses. This review disclosed the advances in the use of urazole as the starting material in the synthesis of various biologically active molecules from 2006 to 2019. Conclusion: Compounds of urazole (1,2,4-triazolidine-3,5-dione) are the most important molecules which are highly active from the biological perspective in the pharmaceuticals as well as polymers. In summary, many protocols for preparations of the urazole derivatives from various substrates in multi-component reactions have been reported from different aromatic and aliphatic groups which have had carbonyl groups in their structures. It is noted that several catalysts have been synthesized to afford applicable molecules with urazole scaffolds. In some papers, being environmentally friendly, short time reactions and high yields are highlighted in the protocols. There is a room to synthesize new catalysts and perform new reactions by manipulating urazole to produce biologically active compounds, even producing chiral urazole component as many groups of chiral urazole compounds are important from biological perspective.

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Ibrahim, Marwa A., Riham F. George, Sahar M. Abou-Seri, and Samir M. El-Moghazy. "Synthesis of new phenolic compounds and biological evaluation as antiproliferative agents." Journal of Chemical Research 44, no. 3-4 (December 16, 2019): 181–92. http://dx.doi.org/10.1177/1747519819895238.

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New series of phenolic azomethine compounds in addition to 5-arylidene thiazolidinones are synthesized and screened for their anticancer activity against the brain cancer cell line SNB-75 and non-small lung cancer cells HOP-92. The azomethine derivative 12b is the most active compound against SNB-75 displaying an IC50 value of 0.14 μM. Compounds 7b, 16a and 27d display submicromolar activity against the HOP-92 cell line with IC50 values of 0.73, 0.74 and 0.81 μM, respectively. Moreover, studying the cytotoxic effects of the most active compounds against normal lung cells WI-38 revealed that compounds 7b, 16a and 27d showed high safety profiles as anticancer agents.

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Ramazani, Ali, Hamed Sadighian, Farideh Gouranlou, and Sang W. Joo. "Syntheses and Biological Activities of triazole-based Sulfonamides." Current Organic Chemistry 23, no. 21 (January 9, 2020): 2319–49. http://dx.doi.org/10.2174/1385272823666191021115023.

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: The triazole and sulfonamide compounds are known as biologically active agents that were employed for medicinal applications. These compounds were obtained in different forms by a variety of techniques to vast ranges of applications. The broad biological properties of these compounds have encouraged researchers to design and synthesize triazole-based sulfonamide derivatives as compounds with potential biological activity. In this review, we summarized the synthetic procedures of triazole-based sulfonamide compounds together with their biological activities during the last two decades.

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Yusupova, Ugiloy Yusufovna, Nurmurod Sheralievich Ramazonov, Khairulla Mamadievich Bobakulov, Feruza Rustamovna Egamova, Vladimir Nikolaevich Syrov, and Durbek Abdikhoshimovich Usmanov. "BIOLOGICAL ACTIVE COMPONENTS OF SILENE TOMENTELLA AND THEIR PHARMACOLOGICAL PROPERTIES." chemistry of plant raw material, no. 1 (March 16, 2021): 197–202. http://dx.doi.org/10.14258/jcprm.2021018323.

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In thepresent investigation isolation of chemical compounds was carried out from the aerial part of Silene tomentella, an evergreen member of the family Caryophyllaceae, using column chromatography. Identification of chemical compounds was done by various MP, TLC, IR, NMR techniques. The presence of the bioactive compound D-pinitol in this plant is being reported for the first time. Under the influence of D-pinitol, a clear tendency towards normalization of the glycogen content in the liver was also noted (it was only 10.4% lower than in intact animals). In the liver of animals, a rather sharp decrease in the content of glycogen was noted – by 63.5%, and a decrease in the activity of enzymes of the antioxidant defense of the body, characteristic of developing diabetes: SOD – by 35.1, and catalase – by 32.4%. Prophylactically – therapeutic administration of D- pinitol, which exhibits a pronounced ability to inhibit free radical oxidation processes.

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Neagu, Mihaela, Daniela Elena Pascu, Gina Alina Traistaru, Georgiana Cretu, Aurelia Cristina Nechifor, Andrei A. Bunaciu, and Hassan Y. Aboul-Enein. "Membrane Separation and Concentration Study of Biological Active Compounds." Analytical Chemistry Letters 3, no. 5-6 (November 2, 2013): 314–21. http://dx.doi.org/10.1080/22297928.2013.861165.

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17

Landau, M. A. "Biological tests of physiologically active compounds (approaches): Communication II." Human Physiology 26, no. 3 (May 2000): 361–65. http://dx.doi.org/10.1007/bf02760200.

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Garaev, Eldar Abdulla, Adila Karam Valiyeva, Amalia Nazim Karamli, and Nigar Mustafa Huseynova. "INVESTIGATION NON-ALKALOIDAL BIOLOGICAL ACTIVE COMPOUNDS OF DATURA INNOXIA." chemistry of plant raw material, no. 2 (June 10, 2021): 163–72. http://dx.doi.org/10.14258/jcprm.2021027947.

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The purpose of the investigation is to study non-alkaloidal biological active compounds of various organs, the antimicrobial activity of plant oil and ethanolic extracts of Datura innoxia Mill. from nightshades (Solanaceae). D. innoxia grows in the natural environmental conditions of the Republic of Azerbaijan. We have studied presence of several biological active compounds – triterpenoic acids, essential oils, fatty acids, sterols and amino acids in the content of various organs of plant. Oil was obtained by using Soxhlet apparatus and investigated by GC method. After removing the oil from the seeds, triterpenoic acids - oleanolic and ursolic acids were isolated and identified by TLC. Essential oils were obtained from plant leaves by hydrodistillation and studied by GC-MS method. 20 amino acids were identified in the aerial part of the plant by the HPLC method, with amino acid analyzer L-8800 (Hitachi, Ltd.), 12 of them are non-essential, 8 are essential. The antimicrobial activity of plant oils of seed and ethanolic extracts of some parts (roots, stems, leaves, flowers, fruits and seeds) were studied on Staphylococcus aureus, Esherichia coli, Pseudomonas aeruginosa, Bacillus anthracoides, Klebsiella pneumoniae and Candida albicans. The significant activity of some extracts (stems, leaves, fruits and seeds) was observed against S. aureus, E. coli, C. albicans, B. anthracoides and plant oil against C. albicans.

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Nakagawa, Toshinori, Ahmed E. Allam, Koichiro Ohnuki, and Kuniyoshi Shimizu. "Biological Activities of Extracts from Different Parts of two Cultivars of Prunus persica ‘Akatsuki’ and ‘Fastigiata’." Natural Product Communications 13, no. 10 (October 2018): 1934578X1801301. http://dx.doi.org/10.1177/1934578x1801301015.

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We investigated the antioxidant, anti-lipase and anti-dementia activities of peach ( Prunus persica (L.) Batsch) fruit and its by-products. The ethanol extracts of branch showed relatively high activity in all biological activities. Then, the extract was fractionated, and eight compounds were isolated from the ethyl acetate fraction. Results showed 4,2’,4'-trihydroxy-6'-methoxychalcone 4'- O-β-D-glucopyranoside (5) and quercetin 3- O-β-D-glucopyranoside (7) as newly identified compounds in P. persica. From the biological investigation, it was considered that quercetin 3- O-β-D-glucopyranoside (7) was the main active compound of antioxidant activity. The main active compound of anti-lipase activity in these was oleanolic acid (1). In addition, (+)-4'- O-methylcatechin (4), 4,2’,4'-trihydroxy-6'-methoxychalcone 4'- O-β-D-glucopyranoside (5) and ferulic acid (6) were the main active compounds of anti-dementia activity with acetylcholinesterase inhibitory assay. The results obtained suggested that these active compounds from peach branches of P. persica could be exploited as natural antioxidants, anti-lipase and anti-dementia materials in the future.

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Kumar Baba, N. H., D. Ashok, Boddu Ananda Rao, Sarasija Madderla, and N. Y. S. Murthy. "Microwave-assisted synthesis and biological evaluation of thiazole-substituted dibenzofurans." Heterocyclic Communications 24, no. 3 (June 27, 2018): 171–76. http://dx.doi.org/10.1515/hc-2017-0247.

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AbstractNew thiazole-substituted dibenzofurans 7a–j were synthesized from dibenzofuran derivatives 5a–b and substituted thiosemicarbazones 6a–h under conventional and microwave irradiation conditions. The structures of all products were established on the basis of analytical and spectral data. The synthesized compounds were evaluated for their in vitro antibacterial activity against Gram-positive and Gram-negative strains. Compounds 7b, 7d and 7h are active against Bacillus subtilis (+ve), and compound 7i displays good activity against Pseudomonas aeruginosa (-ve) strain. Compounds 7a–j were also evaluated for their in vitro antimycobacterial activity, and compound 7b shows antimycobacterial activity against Mycobacterium bovis strain.

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Salakhutdinov, Nariman F., Konstantin P. Volcho, and Olga I. Yarovaya. "Monoterpenes as a renewable source of biologically active compounds." Pure and Applied Chemistry 89, no. 8 (July 26, 2017): 1105–17. http://dx.doi.org/10.1515/pac-2017-0109.

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AbstractMonoterpenes and their derivatives play an important role in the creation of new biologically active compounds including drugs. The review focuses on the data on various types of biological activity exhibited by monoterpenes and their derivatives, including analgesic, anti-inflammatory, anticonvulsant, antidepressant, anti-Alzheimer, anti-Parkinsonian, antiviral, and antibacterial (anti-tuberculosis) effects. Searching for novel potential drugs among monoterpene derivatives shows great promise for treating various pathologies. Special attention is paid to the effect of absolute configuration of monoterpenes and monoterpenoids on their activity.

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Anupam, Anupam, Mohammed Al-Bratty, Hassan Ahmad Alhazmi, Shamim Ahmad, Supriya Maity, Md Shamsher Alam, and Waquar Ahsan. "Synthesis and biological evaluation of triphenyl-imidazoles as a new class of antimicrobial agents." European Journal of Chemistry 9, no. 4 (December 31, 2018): 369–74. http://dx.doi.org/10.5155/eurjchem.9.4.369-374.1785.

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Newer triphenyl-imidazole derivatives (4a-h) were synthesized in good yields by the reaction of benzil and substituted benzaldehydes in equimolar quantities and refluxing the product with acetyl chloride thereafter. Structures were confirmed by using FT-IR, 1H NMR and 13C NMR spectroscopic methods. All the synthesized compounds were tested for their antimicrobial activity using agar diffusion technique against Gram positive (Staphhylococcus aureus and Bacillus subtilis), Gram negative (Escherichia coli and Pseudomonas aureginosa) as well as Fungal strain (Candida albicans). Interestingly compounds 4a, 4b, 4f and 4h showed significant antibacterial activity, whereas compound 4b was found to have remarkable activity against the fungal strain. The Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) of most active compounds were determined by broth dilution method and compound 4b emerged to have potent activities against most of the strains having MIC in the range of 25-200 µg/mL. To check the possible toxicities of the most active compounds, they were orally administered in rats and the concentration of liver enzymes serum glutamic-oxaloacetic transaminase (SGOT), serum glutamic pyruvic transaminase (SGPT) and alkaline phosphatase (ALKP) were determined. Compound 4h showed significant increase in the enzymes level depicting the hepatotoxicity. The structure-activity relationship studies showed the importance of electron withdrawing groups at the distant phenyl ring at ortho and para positions as the compounds having chloro or nitro at these positions tend to be more active than the compounds with electron releasing groups such as methoxy. These compounds may act as lead compounds for further studies and appropriate modification in their structure may lead to agents having high efficacy with lesser toxicity.

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Youssif, Bahaa Gamal Mohamed, and Mostafa H. Abdelrahman. "Synthesis and Biological Evaluation of Some New 1,2,3-Triazole Derivatives As Anti-microbial Agents." JOURNAL OF ADVANCES IN CHEMISTRY 11, no. 2 (January 1, 2016): 3473–84. http://dx.doi.org/10.24297/jac.v11i2.2215.

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A series of 1,2,3-triazole derivatives bearing different chemical entities were prepared starting from 2-(4-phenyl-1H-1,2,3-triazol-1-yl)acetohydrazide, compound 2. The purity of all new compounds was checked by TLC and elucidation of their structures was confirmed by IR, 1H and 13C NMR along with High Resolution Mass Spectrometry (HRMS). All the target compounds were evaluated for their possible antimicrobial activity. Most of the tested compounds showed moderate to good antibacterial activity against most of the bacterial strains used in comparison with ciprofloxacin as a reference drug. The most active compounds were 4a, 9a, 9b, and 9f. Results of antifungal activity revealed that most of the tested compounds showed a good antifungal activity in comparison to fluconazole as a reference drug. Compounds 4a, 9c, 9d and 9f were the most active ones.

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Gadhave, Ranjit V., and Bhanudas S. Kuchekar. "Design, Synthesis and Biological Evaluation of Novel Benzothiazole Based [1,2,4]Triazolo[4,3-c]quinazoline Derivatives." Asian Journal of Chemistry 32, no. 3 (January 31, 2020): 580–86. http://dx.doi.org/10.14233/ajchem.2020.22453.

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A new series of N-(benzo[d]thiazol-2-yl)-[1,2,4]triazolo[4,3-c]quinazoline-5-carboxamide derivatives were synthesized by condensation of [1,2,4]triazolo[4,3-c]quinazoline-5-carboxylate derivatives with substituted benzothiazoles. The chemical structures of the synthesized compounds were confirmed by FT-IR, MS and 1H NMR spectra. Designed triazoloquinazoline derivatives were docked with oxido-reductase enzyme (PDB Code 4h1j) and DNA gyrase enzyme (PDB Code 3g75). Based on high binding affinity score, the best compound were selected for synthesis and subjected to in vitro antioxidant and antibacterial activity. Compounds 7a and 7d were found to be most active compounds as antioxidant agent among this series when compared with ascorbic acid. Compounds 7a, 7d and 7f were found to be most active compounds as an antibacterial agents among this series when compared with ciprofloxacin against bacterial strains such as S. aureus (ATCC 25923), E. coli (ATCC 25922) and P. aeruginosa (ATCC 27853). Study revealed that the most active compounds after structural modifications can be exploited as lead molecules for other pharmacological activities such as anti-inflammatory, anticancer and antidepressant activities.

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Rajak, Harish, Murli Dhar Kharya, and Pradeep Mishra. "Biologically Active 2,5-Disubstituted-1,3,4-Oxadiazoles." International Journal of Pharmaceutical Sciences and Nanotechnology 2, no. 1 (August 31, 2009): 390–406. http://dx.doi.org/10.37285/ijpsn.2009.2.1.2.

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There are vast numbers of pharmacologically active heterocyclic compounds in regular clinical use. The presence of heterocyclic structures in diverse types of compounds is strongly indicative of the profound effects such structure exerts on physiologic activity, and recognition of this is abundantly reflected in efforts to find useful synthetic drugs. The 1,3,4-oxadiazole nucleus has emerged as one of the potential pharmacophore responsible for diverse pharmacological properties. Medical Literature is flooded with reports of a variety of biological activities of 2,5-Disubstituted-1,3,4-oxadiazoles. The present work is an attempt to summarize and enlist the various reports published on biologically active 2,5-disubstituted-1,3,4-oxadiazoles.

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Pakeeraiah, K., Sujit Kumar Mohanty, K. Eswar, and K. Raju. "Azo benzimidazole - A biologically active scaffold." International Journal of PharmTech Research 13, no. 3 (2020): 159–71. http://dx.doi.org/10.20902/ijptr.2019.130305.

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Azo compounds are a very unique class of chemical compounds, drawing considerations in scientific research. Azo compounds are studied as class of organic colorants which have at least a conjugated chromophore azo (-N=N-) group in fusion with one or more aromatic or heterocyclic ring system. Benzimidazole derivatives are privileged intermediates for the development of molecules of pharmaceutical or biological interest. Benzimidazole derivatives have gathered wide applications in diverse therapeutic areas such as antiulcer, anticancer agents, and anthelmintic species to name just a few. Although many azo derivatives of benzimidazole nucleus has been reported in literature but only few of them have been evaluated for their biological potencies. This review focuses primarily on those derivatives which are evaluated as anticancer, antibacterial, antifungal, antitubercular, and other medicinal agents. This review may be helpful for the investigators on the basis of substitution pattern on the nucleus with an objective to assist medicinal chemists for developing an SAR on azo benzimidazoles or similar compounds.

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Hamada, V. R. "Biotechnological aspects of obtaining biologically active substances of Adonis vernalis." Chemistry, Technology and Application of Substances 4, no. 1 (June 1, 2021): 126–30. http://dx.doi.org/10.23939/ctas2021.01.126.

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This article shows the possibility of using a biotechnological method to obtain biologically active compounds based on in vitro cultivation of callus cultures. The callus biomass of Adonis vernalis was obtained in vitro by using the biotechnological method. The extracts based on callus biomass of Adonis vernalis were obtained. The content of flavonoids and phenolic compounds was determined. The antioxidant activity of callus biomass of Adonis vernalis has also been studied. The research results show that the content of biologically active substances and biological activity in callus biomass does not differ from plant raw materials.

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Zhu, Xiaoying, and Renbi Bai. "Separation of Biologically Active Compounds by Membrane Operations." Current Pharmaceutical Design 23, no. 2 (February 13, 2017): 218–30. http://dx.doi.org/10.2174/1381612822666161027153823.

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Background: Bioactive compounds from various natural sources have been attracting more and more attention, owing to their broad diversity of functionalities and availabilities. However, many of the bioactive compounds often exist at an extremely low concentration in a mixture so that massive harvesting is needed to obtain sufficient amounts for their practical usage. Thus, effective fractionation or separation technologies are essential for the screening and production of the bioactive compound products. The applicatons of conventional processes such as extraction, distillation and lyophilisation, etc. may be tedious, have high energy consumption or cause denature or degradation of the bioactive compounds. Membrane separation processes operate at ambient temperature, without the need for heating and therefore with less energy consumption. The “cold” separation technology also prevents the possible degradation of the bioactive compounds. The separation process is mainly physical and both fractions (permeate and retentate) of the membrane processes may be recovered. Thus, using membrane separation technology is a promising approach to concentrate and separate bioactive compounds. Methods: A comprehensive survey of membrane operations used for the separation of bioactive compounds is conducted. The available and established membrane separation processes are introduced and reviewed. Results: The most frequently used membrane processes are the pressure driven ones, including microfiltration (MF), ultrafiltration (UF) and nanofiltration (NF). They are applied either individually as a single sieve or in combination as an integrated membrane array to meet the different requirements in the separation of bioactive compounds. Other new membrane processes with multiple functions have also been developed and employed for the separation or fractionation of bioactive compounds. The hybrid electrodialysis (ED)-UF membrane process, for example has been used to provide a solution for the separation of biomolecules with similar molecular weights but different surface electrical properties. In contrast, the affinity membrane technology is shown to have the advantages of increasing the separation efficiency at low operational pressures through selectively adsorbing bioactive compounds during the filtration process. Conclusion: Individual membranes or membrane arrays are effectively used to separate bioactive compounds or achieve multiple fractionation of them with different molecule weights or sizes. Pressure driven membrane processes are highly efficient and widely used. Membrane fouling, especially irreversible organic and biological fouling, is the inevitable problem. Multifunctional membranes and affinity membranes provide the possibility of effectively separating bioactive compounds that are similar in sizes but different in other physical and chemical properties. Surface modification methods are of great potential to increase membrane separation efficiency as well as reduce the problem of membrane fouling. Developing membranes and optimizing the operational parameters specifically for the applications of separation of various bioactive compounds should be taken as an important part of ongoing or future membrane research in this field.

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Krasnovskaya, Olga, Alexey Naumov, Dmitry Guk, Peter Gorelkin, Alexander Erofeev, Elena Beloglazkina, and Alexander Majouga. "Copper Coordination Compounds as Biologically Active Agents." International Journal of Molecular Sciences 21, no. 11 (May 31, 2020): 3965. http://dx.doi.org/10.3390/ijms21113965.

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Copper-containing coordination compounds attract wide attention due to the redox activity and biogenicity of copper ions, providing multiple pathways of biological activity. The pharmacological properties of metal complexes can be fine-tuned by varying the nature of the ligand and donor atoms. Copper-containing coordination compounds are effective antitumor agents, constituting a less expensive and safer alternative to classical platinum-containing chemotherapy, and are also effective as antimicrobial, antituberculosis, antimalarial, antifugal, and anti-inflammatory drugs. 64Cu-labeled coordination compounds are promising PET imaging agents for diagnosing malignant pathologies, including head and neck cancer, as well as the hallmark of Alzheimer’s disease amyloid-β (Aβ). In this review article, we summarize different strategies for possible use of coordination compounds in the treatment and diagnosis of various diseases, and also various studies of the mechanisms of antitumor and antimicrobial action.

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KAWAHITO, Y., M. KONDO, S. MACHMUDAH, K. SIBANO, M. SASAKI, and M. GOTO. "Supercritical CO2 extraction of biological active compounds from loquat seed." Separation and Purification Technology 61, no. 2 (July 1, 2008): 130–35. http://dx.doi.org/10.1016/j.seppur.2007.09.022.

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Wu, Lei, Zhuoyan Ling, Xueqin Feng, Caiping Mao, and Zhice Xu. "Herb Medicines against Osteoporosis: Active Compounds & Relevant Biological Mechanisms." Current Topics in Medicinal Chemistry 17, no. 15 (April 26, 2017): 1670–91. http://dx.doi.org/10.2174/1568026617666161116141033.

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Christakopoulos, Paul, Io Antonopoulou, and Evangelos Topakas. "Synthesis of biological active compounds using carbohydrate esterases as biocatalysts." New Biotechnology 31 (July 2014): S90—S91. http://dx.doi.org/10.1016/j.nbt.2014.05.1823.

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Mishra, Shweta, Debashree Das, Adarsh Sahu, Shailendra Patil, Ram Kishore Agrawal, and Asmita Gajbhiye. "Phosphonate Derivatives of 3,5-bis(arylidene)-4-piperidone: Synthesis and Biological Evaluation." Anti-Infective Agents 18, no. 3 (September 11, 2020): 245–54. http://dx.doi.org/10.2174/2211352517666190820143735.

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Background: 3,5-Bis(arylidene)-4-piperidinones (BAP) belong to a wide class of cross conjugated dienones. The 1,5-diaryl-3-oxo-1,4-pentadienyl fragment of the BAP moiety is responsible for the molecule's anti-tumor, antioxidant, antimicrobial and anti-inflammatory manifestations. In the present study, we present combinations of phosphonate and 3,5-bis(arylidene)-4- piperidone pharmacophores. The anti-inflammatory, anti-oxidant potential, anti-proliferative, cytotoxic potential and antimicrobial of the title compounds were evaluated in in-vitro bioassay paradigms. Methods: A novel class of phosphonate linked 3,5-Bis(aryl methylene)-4-piperidone derivatives were synthesized from simple, versitalie and efficient synthetic methodology. All of the synthesized compounds were screened for their in vitro anti-inflammatory, in vitro anti-oxidant potential, in vitro anti-proliferative, in vitro cytotoxic potential and in vitro antimicrobial activity. Amongst all the synthesized compounds in series, phosphonate derivatives of 3,5-Bis(arylmethylene)-4- piperidone containing 4-hydroxy-3-methoxyphenyl curcumin like prototype were more active than phenyl substituted compounds. Results: The results of the screening revealed that compounds 5e, 5f, 5g, 5h were more active candidates as compared to 5a, 5b, 5c and 5d, however 5d can be readily endorsed as the most active compound of the series. Structure- activity relationship of the synthesized series suggested that structural resemblance of the synthesized compounds with that of curcumin was enormously accountable for the compounds anti-inflammatory, antioxidant and cytotoxic potential activity. Conclusion: The in-vitro biological spectrum indicated that the substitution of groups at third and fourth position and alkyl phosphonates substitution potentiates the activity as compared to curcumin.

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Lincu, Daniel, Simona Ioniţă, Raul-Augustin Mitran, Mihaela Deaconu, Ana-Maria Brezoiu, Cristian Matei, and Daniela Berger. "Influence of Mesoporous Silica Functionalization and Pore Size on Resveratrol Release Profiles." Proceedings 29, no. 1 (October 11, 2019): 11. http://dx.doi.org/10.3390/proceedings2019029011.

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Kays, Stanley J. "NON-ETHYLENE BIOLOGICALLY ACTIVE POSTHARVEST VOLATILES." HortScience 25, no. 9 (September 1990): 1180f—1180. http://dx.doi.org/10.21273/hortsci.25.9.1180f.

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While we tend to think of postharvest volatiles as nitrogen, oxygen, carbon dioxide and ethylene, harvested products are actually exposed to thousands of volatile compounds. These volatiles are derived from both organic and inorganic sources, evolving from storage room walls, insulation, wrapping materials, combusted products, plants, animals, and a myriad of other sources. Plants alone manufacture a diverse array of secondary metabolizes (estimated to be as many as 400,000) of which many display some degree of volatility. We tend to be cognizant of volatiles when they represent distinct odors. A number of volatiles, however, have significant biological activity, and under appropriate conditions may effect postharvest quality. An overview of biologically active volatile compounds and their relation to postharvest quality will be presented.

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Vanguru, Mahathy, Ramchander Merugu, Swetha Garimella, and Laxminarayana E. "A REVIEW ON THE SYNTHETIC METHODOLOGIES OF CHROMONES." Asian Journal of Pharmaceutical and Clinical Research 11, no. 12 (December 7, 2018): 9. http://dx.doi.org/10.22159/ajpcr.2018.v11i12.27960.

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Chromones group of compounds and their derivatives form the essential component of pharmacophores in many biologically active molecules. They exhibit a wide range of biological activities such as antibiotic, antitumor, antiviral, antioxidant, antipsychotic, and antihypoxic activities. These applications have stimulated a continuous search for the synthesis of new compounds in this field and are being extensively investigated. The various methodologies so far reported for the synthesis of these compounds with the compounds biological applications are discussed in this communication

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Taşkın, Turgut, Eray M. Güler, Şeyda Şentürk, Damla D. Çelik, Turan Arabacı, and Ümran S. Gürer. "Cytotoxic Activity-Guided Isolation from Achillea monocephala, and Biological Activities of its Different Extracts." Open Bioactive Compounds Journal 8, no. 1 (August 18, 2020): 7–14. http://dx.doi.org/10.2174/1874847302008010007.

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Background: The genus Achillea is one of the most important genus of the Asteraceae family and many species of Achillea are used in traditional medicine to treat several ailments. Aim: The aim of the current research was to evaluate in vitro cytotoxic activities of n-hexan, chloroform, ethyl acetate and methanol extracts and to isolate the active compounds from the extract showing the strongest cytotoxic activity. In addition to this, it was aimed to evaluate the biological activities (cytotoxic, antioxidant, anti-urease, anticholinesterase, antimicrobial) of different extracts and active compounds from Achillea monocephala. Methods and Materials: The in vitro antioxidant, cytotoxic, anti-urease, anticholinesterase and antimicrobial activities of different extracts from A. monocephala aerial parts were examined. The structures of the active compounds were determined by NMR techniques, UV, IR and LC-MS/MS analysis and their biological potential was examined. Results: The chloroform extract showed strong and selective cytotoxic activity on the cancer cell lines (MDA-MB-231, MCF-7). Besides, this extract exhibited stronger antimicrobial activity than other extracts. Therefore, through activity-guided procedures, luteolin, naringenin and 8-hydroxy-salvigenin compounds were isolated from this extract. The methanol extract showed stronger antioxidant (DPPH, ABTS, CUPRAC) and anticholinesterase activity than other extracts. The n-hexan extract exhibited the highest anti-urease activity. In this study, it was determined that the isolated compounds had a strong biological activity. Naringenin compound had stronger ABTS radical cation scavenging and ferric reducing/antioxidant power, cytotoxic and antimicrobial activity than other compounds. 8-hydroxy-salvigenin compound showed the highest urease and acetylcholinestease enzyme inhibition. Conclusion: The results of this study suggest that the extracts and isolated compounds from the A. monocephala may be used as antioxidant, cytotoxic, anti-urease, anticholinesterase and antimicrobial agents in the future.

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Arciniegas, Amira, Luis Angel Polindara, Ana L. Pérez-Castorena, Ana María García, Guillermo Avila, José Luis Villaseñor, and Alfonso Romo de Vivar. "Chemical Composition and Biological Activity of Laennecia schiedeana." Zeitschrift für Naturforschung C 66, no. 3-4 (April 1, 2011): 115–22. http://dx.doi.org/10.1515/znc-2011-3-404.

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The chemical study of Laennecia schiedeana afforded three sterols, five diterpenes, five flavonoids, three caffeoyl derivatives of quinic acid, and two triterpenes. Evaluation of the cytotoxic activity of the extracts and isolated metabolites showed that 15-methoxy-16-oxo- 15,16H-strictic acid was the most active compound [(15.05 ± 2.2) μg/mL against U-251 cells]. In antibacterial assays the acetonic extract of leaves was the only active extract exhibiting its highest effect against the multiresistant Staphylococcus epidermidis (MIC 0.25 mg/mL). The anti-inflammatory activity observed was mild in the extracts and not relevant in the isolated compounds

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Sidoryk, Katarzyna, Olga Michalak, Marek Kubiszewski, Andrzej Leś, Marcin Cybulski, Elżbieta U. Stolarczyk, and Jan Doubsky. "Synthesis of Thiol Derivatives of Biological Active Compounds for Nanotechnology Application." Molecules 25, no. 15 (July 30, 2020): 3470. http://dx.doi.org/10.3390/molecules25153470.

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An efficient method of thiol group introduction to the structure of common natural products and synthetic active compounds with recognized biological efficacy such genistein (1), 5,11-dimethyl-5H-indolo[2,3-b]quinolin (2), capecitabine (3), diosgenin (4), tigogenin (5), flumethasone (6), fluticasone propionate (7), ursolic acid methyl ester (8), and β-sitosterol (9) was developed. In most cases, the desired compounds were obtained easily via two-step processes involving esterification reaction employing S-trityl protected thioacetic acid and the corresponding hydoxy-derivative, followed by removal of the trityl-protecting group to obtain the final compounds. The results of our preliminary experiments forced us to change the strategy in the case of genistein (1), and the derivatization of diosgenin (4), tigogenin (5), and capecitabine (3) resulted in obtaining different compounds from those designed. Nevertheless, in all above cases we were able to obtain thiol-containing derivatives of selected biological active compounds. Moreover, a modelling study for the two-step thiolation of genistein and some of its derivatives was accomplished using the density functional theory (B3LP). A hypothesis on a possible reason for the unsuccessful deprotection of the thiolated genistein is also presented based on the semiempirical (PM7) calculations. The developed methodology gives access to new sulphur derivatives, which might find a potential therapeutic benefit.

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Al-Sheikh, Ahmed, Masuma Begum, Bian Zhang, Richard A. Lewis, Nicholas E. E. Allenby, Paul G. Waddell, and Bernard T. Golding. "Molecular Diversity via Tetrasubstituted Alkenes Containing a Barbiturate Motif: Synthesis and Biological Activity." Molecules 25, no. 24 (December 11, 2020): 5868. http://dx.doi.org/10.3390/molecules25245868.

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The synthesis of a molecularly diverse library of tetrasubstituted alkenes containing a barbiturate motif is described. Base-induced condensation of N1-substituted pyrimidine-2,4,6(1H,3H,5H)-triones with 5-(bis(methylthio)methylene)-2,2-dimethyl-1,3-dioxane-4,6-dione gave 3-substituted 5-(methylthio)-2H-pyrano[2,3-d]pyrimidine-2,4,7(1H,3H)-triones (‘pyranopyrimidinones’), regioselectively. A sequence of reactions involving ring-opening of the pyran moiety, displacement of the methylthio group with an amine, re-formation of the pyran ring, and after its final cleavage with an amine, gave tetrasubstituted alkenes (3-amino-3-(2,4,6-trioxotetrahydropyrimidin-5(2H)-ylidene)propanamides) with a diversity of substituents. Cleavage of the pyranopyrimidinones with an aniline was facilitated in 2,2,2-trifluoroethanol under microwave irradiation. Compounds were tested against Escherichia coli, Staphylococcus aureus, the yeast Schizosaccharomyces pombe, and the pathogenic fungus Candida albicans. No compounds exhibited activity against E. coli, whilst one compound was weakly active against S. aureus. Three compounds were strongly active against S. pombe, but none was active against C. albicans.

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Ruwizhi, Ngonidzashe, and Blessing Atim Aderibigbe. "Cinnamic Acid Derivatives and Their Biological Efficacy." International Journal of Molecular Sciences 21, no. 16 (August 9, 2020): 5712. http://dx.doi.org/10.3390/ijms21165712.

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The role played by cinnamic acid derivatives in treating cancer, bacterial infections, diabetes and neurological disorders, among many, has been reported. Cinnamic acid is obtained from cinnamon bark. Its structure is composed of a benzene ring, an alkene double bond and an acrylic acid functional group making it possible to modify the aforementioned functionalities with a variety of compounds resulting in bioactive agents with enhanced efficacy. The nature of the substituents incorporated into cinnamic acid has been found to play a huge role in either enhancing or decreasing the biological efficacy of the synthesized cinnamic acid derivatives. Some of the derivatives have been reported to be more effective when compared to the standard drugs used to treat chronic or infectious diseases in vitro, thus making them very promising therapeutic agents. Compound 20 displayed potent anti-TB activity, compound 27 exhibited significant antibacterial activity on S. aureus strain of bacteria and compounds with potent antimalarial activity are 35a, 35g, 35i, 36i, and 36b. Furthermore, compounds 43d, 44o, 55g–55p, 59e, 59g displayed potent anticancer activity and compounds 86f–h were active against both hAChE and hBuChE. This review will expound on the recent advances on cinnamic acid derivatives and their biological efficacy.

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Lazic, Anita, Natasa Valentic, Nemanja Trisovic, Slobodan Petrovic, and Gordana Uscumlic. "Synthesis, structure and biological properties of active spirohydantoin derivatives." Chemical Industry 70, no. 2 (2016): 177–99. http://dx.doi.org/10.2298/hemind150205025l.

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Spirohidantoins represent an pharmacologically important class of heterocycles since many derivatives have been recognized that display interesting activities against a wide range of biological targets. First synthesis of cycloalkanespiro-5-hydantoins was performed by Bucherer and Lieb 1934 by the reaction of cycloalkanone, potassium cyanide and ammonium-carbonate at reflux in a mixture of ethanol and water. QSAR (Quantitative Structure-Activity Relationship) studies showed that a wide range of biological activities of spirohydantoin derivatives strongly depend upon their structure. This paper describes different methods of synthesis of spirohydantoin derivatives, their physico-chemical properties and biological activity. It emphasizes the importance of cycloalkanespiro-5-hydantoins with anticonvulsant, antiproliferative, antipsychotic, antimicrobial and antiinflammatory properties as well as their importance in the treatment of diabetes. Numerous spirohydantoin compounds exhibit physiological activity such as serotonin and fibrinogen antagonist, inhibitors of the glycine binding site of the NMDA receptor also, antagonist of leukocyte cell adhesion, acting as allosteric inhibitors of the protein-protein interactions. Some spirohydantoin derivatives have been identified as antitumor agents. Their activity depends on the substituent presented at position N-3 of the hydantoin ring and increases in order alkene > ester > ether. Besides that, compounds that contain two electron withdrawing groups (e.g. fluorine or chlorine) on the third and fourth position of the phenyl ring are better antitumor agents than compounds with a single electron withdrawing group.

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Insuasty, Daniel, Juan Castillo, Diana Becerra, Hugo Rojas, and Rodrigo Abonia. "Synthesis of Biologically Active Molecules through Multicomponent Reactions." Molecules 25, no. 3 (January 24, 2020): 505. http://dx.doi.org/10.3390/molecules25030505.

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Focusing on the literature progress since 2002, the present review explores the highly significant role that multicomponent reactions (MCRs) have played as a very important tool for expedite synthesis of a vast number of organic molecules, but also, highlights the fact that many of such molecules are biologically active or at least have been submitted to any biological screen. The selected papers covered in this review must meet two mandatory requirements: (1) the reported products should be obtained via a multicomponent reaction; (2) the reported products should be biologically actives or at least tested for any biological property. Given the diversity of synthetic approaches utilized in MCRs, the highly diverse nature of the biological activities evaluated for the synthesized compounds, and considering their huge structural variability, much of the reported data are organized into concise schemes and tables to facilitate comparison, and to underscore the key points of this review.

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Rostas, Arpad Mihai, Mihaela Badea, Lavinia L. Ruta, Ileana C. Farcasanu, Catalin Maxim, Mariana Carmen Chifiriuc, Marcela Popa, et al. "Copper(II) Complexes with Mixed Heterocycle Ligands as Promising Antibacterial and Antitumor Species." Molecules 25, no. 17 (August 19, 2020): 3777. http://dx.doi.org/10.3390/molecules25173777.

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Complexes with mixed ligands [Cu(N-N)2(pmtp)](ClO4)2 ((1) N-N: 2,2′-bipyridine; (2) L: 1,10-phenanthroline and pmpt: 5-phenyl-7-methyl-1,2,4-triazolo[1,5-a]pyrimidine) were synthesized and structurally and biologically characterized. Compound (1) crystallizes into space group Pa and (2) in P-1. Both complexes display an intermediate stereochemistry between the two five-coordinated ones. The biological tests indicated that the two compounds exhibited superoxide scavenging capacity, intercalative DNA properties, and metallonuclease activity. Tests on various cell systems indicated that the two complexes neither interfere with the proliferation of Saccharomyces cerevisiae or BJ healthy skin cells, nor cause hemolysis in the active concentration range. Nevertheless, the compounds showed antibacterial potential, with complex (2) being significantly more active than complex (1) against all tested bacterial strains, both in planktonic and biofilm growth state. Both complexes exhibited a very good activity against B16 melanoma cells, with a higher specificity being displayed by compound (1). Taken together, the results indicate that complexes (1) and (2) have specific biological relevance, with potential for the development of antitumor or antimicrobial drugs.

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Solecka, Jolanta, Joanna Zajko, Magdalena Postek, and Aleksandra Rajnisz. "Biologically active secondary metabolites from Actinomycetes." Open Life Sciences 7, no. 3 (June 1, 2012): 373–90. http://dx.doi.org/10.2478/s11535-012-0036-1.

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AbstractSecondary metabolites obtained from Actinomycetales provide a potential source of many novel compounds with antibacterial, antitumour, antifungal, antiviral, antiparasitic and other properties. The majority of these compounds are widely used as medicines for combating multidrug-resistant Gram-positive and Gram-negative bacterial strains. Members of the genus Streptomyces are profile producers of previously-known secondary metabolites. Actinomycetes have been isolated from terrestrial soils, from the rhizospheres of plant roots, and recently from marine sediments. This review demonstrates the diversity of secondary metabolites produced by actinomycete strains with respect to their chemical structure, biological activity and origin. On the basis of this diversity, this review concludes that the discovery of new bioactive compounds will continue to pose a great challenge for scientists.

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Feldmann, Christian, Dimitar Yonchev, and Jürgen Bajorath. "Structured data sets of compounds with multi-target and corresponding single-target activity from biological assays." Future Science OA 7, no. 5 (June 2021): FSO685. http://dx.doi.org/10.2144/fsoa-2020-0209.

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Aim: Providing compound data sets for promiscuity analysis with single-target (ST) and multi-target (MT) activity, taking confirmed inactivity against targets into account. Methodology: Compounds and target annotations are extracted from screening assays. For a given combination of targets, MT and ST compounds are identified, ensuring test data completeness. Exemplary results & data: A total of 1242 MT compounds active against five or more targets and 6629 corresponding ST compounds are characterized, organized and made freely available. Limitations & next steps: Screening campaigns typically cover a smaller target space than compounds from the medicinal chemistry literature and their activity annotations might be of lesser quality. Reported compound groups will be subjected to target set-based promiscuity analysis and predictions.

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Kuznetsov, Dmitry N., Konstantin I. Kobrakov, Anna G. Ruchkina, and Galina S. Stankevich. "BIOLOGICALLY ACTIVE SYNTHETIC ORGANIC DYES." IZVESTIYA VYSSHIKH UCHEBNYKH ZAVEDENIY KHIMIYA KHIMICHESKAYA TEKHNOLOGIYA 60, no. 1 (March 1, 2017): 4. http://dx.doi.org/10.6060/tcct.2017601.5423.

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For citation:Kuznetsov D.N., Kobrakov K.I., Ruchkina A.G., Stankevich G.S. Biologically active synthetic organic dyes. Izv. Vyssh. Uchebn. Zaved. Khim. Khim. Tekhnol. 2017. V. 60. N 1. P. 4-33.This review is based on the publications found in CAS (Chemical Abstracts Service) database available from STN (The Scientific and Technical Information Network) with respect to dyes, and the compounds that can be classified as the dyes molecular variants. The substances were categorised based on the dyes chromophore properties. Special care was taken to determine the “composition - property” profile within the range of structurally similar compounds. An extensive list of literature references is provided to support the review's subject, including the authors’ own studies on the synthesis, properties and applications of coloured biologically active compounds. The view covers the uses of coloured biologically active compounds as textile dyes and the uses in other industries such as medical, agricultural etc. The review is substantially focused on biocidal azo dyes for the reason of the great variety of possible diazo and azo components which are used for the synthesis of dyes to create an abundance of biocidal dyes with a wide scale of colors. Usage of dyes which add expressed biocidal properties to the coloured textile and other materials and make them resistent to physical and chemical agents is a subject of obvious practical interest, as this enables the combination of two manufacturing processes in one step: coloration and special chemical treatment. Moreover, as it appears from the review, biocidal dyes may be used as additives to the primary dye, without affecting the colour of the object being dyed, albeit in quantities sufficient to endow the required biocidal properties. As demonstated by the review, streamlined synthesis of textile dyes exhibiting biocidal properties, which are able to make a material resistent to biodeterioration or add medicinal properties to the material, is hard to accomplish due to the lack of profound understanding of the mode of action of such compounds. However, the available “composition - property” data and the computer-aided screening data of the biological activity of organic compounds allow us to model and synthesise target products with a high degree of confidence. The review doesn’t cover the properties of biocidal dyes derived from natural raw materials.

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Khan, Hamayun, Hazrat Amin, Asad Ullah, Sumbal Saba, Jamal Rafique, Khalid Khan, Nasir Ahmad, and Syed Lal Badshah. "Antioxidant and Antiplasmodial Activities of Bergenin and 11-O-Galloylbergenin Isolated fromMallotus philippensis." Oxidative Medicine and Cellular Longevity 2016 (2016): 1–6. http://dx.doi.org/10.1155/2016/1051925.

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Two important biologically active compounds were isolated fromMallotus philippensis. The isolated compounds were characterized using spectroanalytical techniques and found to be bergenin (1) and 11-O-galloylbergenin (2). Thein vitroantioxidant and antiplasmodial activities of the isolated compounds were determined. For the antioxidant potential, three standard analytical protocols, namely, DPPH radical scavenging activity (RSA), reducing power assay (RPA), and total antioxidant capacity (TAC) assay, were adopted. The results showed that compound2was found to be more potent antioxidant as compared to1. Fascinatingly, compound2displayed better EC50results as compared toα-tocopherol while being comparable with ascorbic acid. The antiplasmodial assay data showed that both the compound exhibited good activity against chloroquine sensitive strain ofPlasmodium falciparum(D10) and IC50values were found to be less than 8 μM. Thein silicomolecular docking analyses were also performed for the determination of binding affinity of the isolated compounds usingP. falciparumproteins PfLDH and Pfg27. The results showed that compound2has high docking score and binding affinity to both protein receptors as compared to compound1. The demonstrated biological potentials declared that compound2could be the better natural antioxidant and antiplasmodial candidate.

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Journal, Baghdad Science. "Studying the biological activity of some Antimony Compounds with amino acids." Baghdad Science Journal 7, no. 1 (March 7, 2010): 431–36. http://dx.doi.org/10.21123/bsj.7.1.431-436.

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In this work four complexes of antimony were prepared ,Na[SbO(gly)2],Na[SbO(Asp)2],Na[SbO(Tyrosin)2], Na [SbO(phen alanin)2]. by reaction SbOCl with salts amino acids identifiefid these complexes by FTIR ,their conductivity was measured and also their biological activity against two types of bacteria was studied ,they were biologically active.

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Sharma, Piush, and Charanjeet Singh. "Synthesis, characterization and biological evaluation of some novel N-Mannich bases of heterocyclic 1,3,4-thiadiazole." Journal of Drug Delivery and Therapeutics 9, no. 4-A (August 30, 2019): 220–28. http://dx.doi.org/10.22270/jddt.v9i4-a.3332.

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A series of some novel N-Mannich bases of heterocyclic 1,3,4-thiadiazole were synthesized through the condensation reaction of 1,3,4-thiadiazole containing a aromatic secondary amine, aromatic aldehydes and cyclic compounds employing Mannich reaction and using conventional synthesis. All the synthesized compounds were obtained in the range of 57.41-83.3 % yield. The structures of synthesized compounds were confirmed by UV, IR, 1H NMR spectroscopy. the essential structural features responsible for interaction with receptor site are established within a suggested pharmacophore. The in vitro antibacterial activity of the synthesized compounds was determined, against two Gram-positive bacteria, viz. S. aureus & B. subtilis and Gram-negative, viz. E. coli and K. pneumoniae, by cup-plate method using the standard drug ciprofloxacin. Minimum inhibitory concentrations (MIC) changed in the range of 1.56_ _ 200 mg mL_1. Compound 3b exhibited excellent activity against both bacteria. The in vitro antifungal activity of the synthesized compound was also evaluated by cup-plate method against the fungi A. niger and C. albicans compared with the standard drug Fluconazole. Compound 4a, 8a exhibited excellent activity against both fungi. The result has shown that the compounds are quite active against pathogens under study and were nontoxic. The anti-inflammatory activity of the compound was evaluated, on albino rats, by carageenan induced rat paw oedema method using the standard drug diclofenac sodium. Compound 7b and 8c exhibited excellent anti-inflammatory and analgesic pharmacological activities. Structurally the compound 7b has a greater number of unsaturated hydrocarbons in schiff base, which shows good lipophilic properties within electron rich morpholine ring in Mannich base. Statistical significance of differences between group was determined by one-way analysis of variance (ANOVA). Among the synthesized compounds 3a, 4b, 5c, 7b, 8a and 8c were found be the most active. All the synthesized compounds were found to be low lethal as ascertained by LD50 test. Keywords: N- Mannich bases of heterocyclic 1,3,4-thiadiazole derivatives; Mannich reaction; antimicrobial agents; anti-inflammatory activity;

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Journal articles on the topic 'Biological active compounds'

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