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Journal articles on the topic 'Bioactive compounds - Synthesis'

Author: Grafiati

Published: 4 June 2021

Last updated: 25 January 2023

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1

Suryaningtyas, Indyaswan Tegar. "SENYAWA BIOAKTIF MIKROALGA DAN PROSPEKNYA DI MASA DEPAN." OSEANA 44, no. 1 (April 30, 2019): 15–25. http://dx.doi.org/10.14203/oseana.2019.vol.44no.1.28.

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BIOACTIVE COMPOUND FROM MICROALGAE AND ITS FUTURE PROSPECT. Microalgae biomass is potential to be used in various fields, one of which is as a producer of bioactive compounds. Bioactive compounds from microalgae can be used extensively in the pharmaceutical industry, cosmetic’s raw materials, food flavouring substances, and functional food ingredients. In terms of health, the bioactive compounds have the potential as antioxidants, antiviral, antibacterial, anti-fungal, anti-inflammatory, anti-tumor, and prevent the effects of malaria, but the potential for microalgae’s bioactive compound has not been explored well if compared to the production of terrestrial plants. Some examples of the bioactive compounds that have been used are carotenoid groups such as lutein, β-carotene, astaxanthin and fucoxanthin; fatty acid groups such as EPA and DHA; and also some toxin compounds such as domoic acid. To obtain the optimum yield of bioactive compounds, it requires the right method in biomass production, compound extraction, compounds isolation and compounds identification. While testing the activities, it is necessary to do some assays such as antioxidan, antibiotic, antiviral and anticancer assay. The development of the technology can improve the potential use of microalgae to synthesis its bioactive compounds.

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2

Trabocchi, Andrea. "Design and synthesis of bioactive compounds." Bioorganic & Medicinal Chemistry 25, no. 19 (October 2017): 5031. http://dx.doi.org/10.1016/j.bmc.2017.09.020.

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3

Susanto, Edy, Anik Fadlilah, and Muhammad Fathul Amin. "Synthesis, extraction and idetification of meat bioactive peptides: a review." IOP Conference Series: Earth and Environmental Science 888, no. 1 (November 1, 2021): 012058. http://dx.doi.org/10.1088/1755-1315/888/1/012058.

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Abstract The consumption of meat should consider the concept of functional food. The meat had a highquality protein and contain of bioactive peptide compounds. Amino acid was component of bioactive peptides compound. It joined by covalent bonds known as amide or peptide bonds. A lot of research was currently focused on the bioactive peptide compounds isolated from myofibril and sarcoplasmic proteins with the synthesis, extraction, and identification methods. This study used a systematic review to get the structure of amino acids that the source of bioactive components and the principle of synthesis, extraction and identification of bioactive peptide in the meat. This paper highlights were finding on the structure of amino acid in the meat. The proportion of amino acids was also different in each animal body location. The result identified that more than 170 peptides were released from the main structure of the myofibril (actin, myosin) and sarcoplasmic muscle proteins, and the synthesis, extraction and bioactive peptide identification in the meat as well as their potential use as functional food.

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4

Tatsuta, Kuniaki. "Significance of Total Synthesis of Bioactive Compounds." Current Organic Chemistry 5, no. 2 (February 1, 2001): 207–31. http://dx.doi.org/10.2174/1385272013375670.

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5

ISOBE, Minoru. "Stereocontrolled Synthesis of Multi-Functional Bioactive Compounds." Journal of Synthetic Organic Chemistry, Japan 55, no. 1 (1997): 44–55. http://dx.doi.org/10.5059/yukigoseikyokaishi.55.44.

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6

Resnati, Giuseppe. "Synthesis of chiral and bioactive fluoroorganic compounds." Tetrahedron 49, no. 42 (1993): 9385–445. http://dx.doi.org/10.1016/s0040-4020(01)80212-x.

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7

Garcı́a-Junceda, Eduardo, Juan Francisco Garcı́a-Garcı́a, Agatha Bastida, and Alfonso Fernández-Mayoralas. "Enzymes in the synthesis of bioactive compounds." Bioorganic & Medicinal Chemistry 12, no. 8 (April 2004): 1817–34. http://dx.doi.org/10.1016/j.bmc.2004.01.032.

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8

Melford C Egbujor, Uchechukwu C Okoro, Samuel A Egu, Pius I Egwuatu, Florence U Eze, and Ifeanyi S Amasiatu. "Synthesis and Biological Evaluation of Alanine Derived Bioactive p-Toluenesulphonamide Analogs." International Journal of Research in Pharmaceutical Sciences 11, no. 4 (October 19, 2020): 6449–58. http://dx.doi.org/10.26452/ijrps.v11i4.3440.

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Sulphonamides and carboxamides have great pharmacological importance. The purpose of the study was to synthesize alanine-derived bioactive sulphonamides bearing carboxamides and evaluate their biological activities. The reaction of p-toluenesulphonyl chloride with L-alanine afforded compound 1, which was acetylated to obtain compound 2. The chlorination and ammonolysis of compound 2 gave the carboxamide backbone (3) which was coupled with aryl/heteroaryl halides to afford the hybrid compounds 4, 5 and 6. Structures were confirmed by FTIR, 1H-NMR, 13C-NMR spectra and elemental analytical data. The in vitro antimicrobial properties were determined by agar dilution, and the antioxidant properties were also investigated. Molecular docking interactions of the analogues were determined using PyRx. Compounds 4, 5 and 6 exhibited excellent in vitro antimicrobial properties in the range of 0.5-1.0mg/ml while compounds 1and 2 had half-maximal inhibitory concentration (IC50) of 1.11±0.15µg/ml and 1.12±0.13µg/ml respectively. For the molecular docking studies, compounds 5 and 6 displayed the best antitrypanosomal activity with binding affinities of -13.95 and -13.51kcal/mol respectively while compound 4 showed the highest in silico antimalarial activity having binding affinity of -11.95kcal/mol. All the alanine derived sulphonamides were observed to be potential antimicrobial, antioxidant, antitrypanosomal and antimalarial agents following the biological activities studies.

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9

Lee, Hing-Ken, Kin-Fai Chan, Chi-Wai Hui, Ho-Kee Yim, Xun-Wei Wu, and Henry N. C. Wong. "Use of furans in synthesis of bioactive compounds." Pure and Applied Chemistry 77, no. 1 (January 1, 2005): 139–43. http://dx.doi.org/10.1351/pac200577010139.

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Synthetic approaches to the total synthesis of plakortone B, as well as diastereoselective nucleophilic additions to furyl aldehyde and furyl sulfonylimine employing chiral 3-boronates as auxiliary are presented.

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10

Khan, Ayad Kareem, Suaad Mohammed Hussain, Mohammed Rifat Ahmad, Fitua Manwar Aziz, and Shimaa Mutasim Abdulah***. "Synthesis, Characterization and Antimicrobial Screening of Some Bioactive 1,8-Naphthalimide Derivatives." Al Mustansiriyah Journal of Pharmaceutical Sciences 14, no. 2 (December 1, 2014): 33–47. http://dx.doi.org/10.32947/ajps.v14i2.145.

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This research include developing new heterocyclic derivatives of 1,8-naphthalimides bearing oxazoline, thiazoline, oxadiazole, thiadiazole and aminotriazole moieties as the following steps: N-ester-1,8-naphthalimide (1) was obtained by direct imidation of 1,8- naphthalic anhydride with ethylglycinate in dimethylsulfoxide. Compound (1) was treated with hydrazine hydrate in absolute ethanol to give N-acetohydrazide-1,8-naphthalimide (2).N-Acetophenylsemicarbazide-1,8-naphthalimide (3) and N-Aceto phenylthiosemicarbazide- 1,8-naphthalimide (7) were synthesized via reaction of compound (2) with phenylisocyanate and phenylisothiocyanate in absolute ethanol respectively.Cyclization of compounds (3) and (7) with p-substituted phenacyl bromide gives the oxazoline derivatives (4-6) and thiazoline derivatives (9-11) respectively. N-Methyl-[(5- (phenyl amino)-1,3,4-thiadiazol-2-yl)]-1,8-naphthalimide (8) prepared via treatment of compound (7) with phosphoric acid. Reaction of the prepared hydrazide (2) with carbon disulfide in the presence of potassium hydroxide producing N-Methyl-[potassium dithiocarbazate]-1,8-naphthalimide (12). Acidifying of the obtained salt (12) with 4N hydrochloric acid give N-Methyl-[1,3,4-oxadiazol-2-yl-5-thiol]-1,8-naphthalimide (13). The obtained salt (12) also treated with hydrazine hydrate to afford the desirable N-Methyl-[1,2,4- triazol-3-yl-4-amino-5-thiol]-1,8-naphthalimide (14).All the prepared compounds in this research were characterized by recording their melting points, FTIR, 1HNMR, 13CNMR spectra, checked by TLC, physical properties and some specific chemical tests also. Some of the new prepared compounds were evaluated for the antimicrobial screening in vitro against two types of Gram positive bacteria including (Staphylococcus aureus, Bacillus subtilis) and two types of Gram negative bacteria including (Escherichia coli, Pseudomonas aeuroginosa).More, antifungal activities of some prepared compounds performed against the yeastlike pathogenic fungus (Candida albicans). The antimicrobial screening carried out in three concentrations of prepared compounds. Sulfamethoxazole/Clotrimazole was used as standard drugs. The results showed that most of the tested compounds have good biological activity against the mentioned organisms compared with standard drugs above

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11

Kunig, Verena, Marco Potowski, Anne Gohla, and Andreas Brunschweiger. "DNA-encoded libraries – an efficient small molecule discovery technology for the biomedical sciences." Biological Chemistry 399, no. 7 (June 27, 2018): 691–710. http://dx.doi.org/10.1515/hsz-2018-0119.

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Abstract DNA-encoded compound libraries are a highly attractive technology for the discovery of small molecule protein ligands. These compound collections consist of small molecules covalently connected to individual DNA sequences carrying readable information about the compound structure. DNA-tagging allows for efficient synthesis, handling and interrogation of vast numbers of chemically synthesized, drug-like compounds. They are screened on proteins by an efficient, generic assay based on Darwinian principles of selection. To date, selection of DNA-encoded libraries allowed for the identification of numerous bioactive compounds. Some of these compounds uncovered hitherto unknown allosteric binding sites on target proteins; several compounds proved their value as chemical biology probes unraveling complex biology; and the first examples of clinical candidates that trace their ancestry to a DNA-encoded library were reported. Thus, DNA-encoded libraries proved their value for the biomedical sciences as a generic technology for the identification of bioactive drug-like molecules numerous times. However, large scale experiments showed that even the selection of billions of compounds failed to deliver bioactive compounds for the majority of proteins in an unbiased panel of target proteins. This raises the question of compound library design.

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12

Yang, Fei, Mingyan Zhu, Jinyi Zhang, and Huchen Zhou. "Synthesis of biologically active boron-containing compounds." MedChemComm 9, no. 2 (2018): 201–11. http://dx.doi.org/10.1039/c7md00552k.

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13

TATSUTA, Kuniaki. "Total Synthesis and Development of Useful Bioactive Compounds." Journal of Synthetic Organic Chemistry, Japan 56, no. 9 (1998): 714–24. http://dx.doi.org/10.5059/yukigoseikyokaishi.56.714.

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14

Abdel Hafez, O., Kh Ahmed, and E. Haggag. "Synthesis of Some Potentially Bioactive Compounds From Visnaginone." Molecules 6, no. 4 (March 31, 2001): 396–405. http://dx.doi.org/10.3390/60400396.

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15

Kudanga, Tukayi, Blessing Nemadziva, and Marilize Le Roes-Hill. "Laccase catalysis for the synthesis of bioactive compounds." Applied Microbiology and Biotechnology 101, no. 1 (November 21, 2016): 13–33. http://dx.doi.org/10.1007/s00253-016-7987-5.

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16

Dallinger, Doris, A. Stadler, and C. O. Kappe. "Solid- and solution-phase synthesis of bioactive dihydropyrimidines." Pure and Applied Chemistry 76, no. 5 (January 1, 2004): 1017–24. http://dx.doi.org/10.1351/pac200476051017.

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With the emergence of high-throughput screening in the pharmaceutical industry over a decade ago, synthetic chemists were faced with the challenge of preparing large collections of molecules to satisfy the demand for new screening compounds. The unique exploratory power of multicomponent reactions such as the Biginelli three-component reaction was soon recognized to be extremely valuable to produce compound libraries in a time- and cost-effective manner. The present review summarizes synthetic advances from our laboratories for the construction of Biginelli libraries via solution-and solid-phase strategies that are amenable to a high-throughput or combinatorial format.

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17

Menéndez, J., Marco Leonardi, Verónica Estévez, and Mercedes Villacampa. "The Hantzsch Pyrrole Synthesis: Non-conventional Variations and Applications of a Neglected Classical Reaction." Synthesis 51, no. 04 (December 3, 2018): 816–28. http://dx.doi.org/10.1055/s-0037-1610320.

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Pyrrole is one of the most important one-ring heterocycles because of its widespread presence in natural products and unnatural bioactive compounds and drugs in clinical use. The preparation of pyrroles by reaction between primary amines, β-dicarbonyl compounds, and α-halo ketones, known as the Hantzsch pyrrole synthesis, is reviewed here for the first time. In spite of its age and its named reaction status, this method has received little attention in the literature. Recent work involving the use of non-conventional conditions has rejuvenated this classical reaction and this is emphasized in this review. Some applications of the Hantzsch reaction in target-oriented synthesis are also discussed.1 Introduction2 The Conventional Hantzsch Pyrrole Synthesis3 Hantzsch Pyrrole Synthesis under Non-conventional Conditions4 Applications of the Hantzsch Pyrrole Synthesis5 Conclusions

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18

Arshad, Tanzila, Hamdullah Khadim Sheikh, Mehdi Hassan Kazmi, Sadia Farheen, Tehmina Sohail, and Mehreen Lateef. "New bioactive triaryl triglyceride esters: Synthesis, characterization and biological activities." Bangladesh Journal of Pharmacology 13, no. 4 (October 14, 2018): 302. http://dx.doi.org/10.3329/bjp.v13i4.37210.

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<p class="Abstract">Four new bioactive aryl triester derivatives of glycerol and benzoic acids were synthesized. The synthetic compounds were studied for their antimicrobial and urease inhibition activities. Esterification was carried out by using carbonyldiimidazole to enhance the acyl elimination addition reaction with benzoic acid derivatives. The structure of triglycerides were studied by EI-MS, <sup>1</sup>H, <sup>13</sup>C-NMR, FT-IR and elemental analysis. All synthetic compounds showed urease inhibition activity with highest value of IC<sub>50 </sub>value 22.4 ± 0.45 μM which is nearest to standard thiourea IC<sub>50 </sub>value (21.6 ± 0.12 μM). Except compound (3d), all other compounds exhibited antimicrobial activity against <em>Streptococcus pneumoniae, Staphylococcus epidermidis, Bacillus pumilus, Escherichia coli, Pseudomonas aeruginosa</em> and <em>Candida albican</em>.</p><p><strong>Video Clip of Methodology:</strong></p><p>7 min 59 sec <a href="https://youtube.com/v/PvGTYUxO7-4">Full Screen</a> <a href="https://youtube.com/watch?v=PvGTYUxO7-4">Alternate</a> </p>

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19

Graebin, Cedric S., Felipe V. Ribeiro, Kamilla R. Rogério, and Arthur E. Kümmerle. "Multicomponent Reactions for the Synthesis of Bioactive Compounds: A Review." Current Organic Synthesis 16, no. 6 (November 26, 2019): 855–99. http://dx.doi.org/10.2174/1570179416666190718153703.

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Multicomponent reactions (MCRs) are composed of three or more reagents in which the final product has all or most of the carbon atoms from its starting materials. These reactions represent, in the medicinal chemistry context, great potential in the research for new bioactive compounds, since their products can present great structural complexity. The aim of this review is to present the main multicomponent reactions since the original report by Strecker in 1850 from nowadays, covering their evolution, highlighting their significance in the discovery of new bioactive compounds. The use of MCRs is, indeed, a growing field of interest in the synthesis of bioactive compounds and approved drugs, with several examples of commerciallyavailable drugs that are (or can be) obtained through these protocols.

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20

Abd Samat, Nur Mardhiati Afifa, Syahida Ahmad, Yahya Awang, Ros Azrinawati Hana Bakar, and Mansor Hakiman. "Alterations in Herbage Yield, Antioxidant Activities, Phytochemical Contents, and Bioactive Compounds of Sabah Snake Grass (Clinacanthus Nutans L.) with Regards to Harvesting Age and Harvesting Frequency." Molecules 25, no. 12 (June 19, 2020): 2833. http://dx.doi.org/10.3390/molecules25122833.

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Sabah snake grass or Clinacanthus nutans has drawn public interest having significant economic benefits attributable to the presence of phytochemicals and several interesting bioactive constituents that may differ according to harvesting age and harvesting frequency. The current study was aimed to evaluate the effect of harvesting age and harvesting frequency towards herbal yield, antioxidant activities, phytochemicals synthesis, and bioactive compounds of C. nutans. A factorial randomized completely block design with five replications was used to illustrate the relationship between herbal yield, DPPH (2, 2-diphenyl-1-picrylhydrazyl) and ferric reducing antioxidant power (FRAP) assays, total phenolic and flavonoid content affected by harvesting age (week 8, 12, and 16 after transplanting), and harvesting frequency (harvest 1, 2, and 3). The bioactive compounds by HPLC were also determined to describe the interaction effect between both harvesting age and harvesting frequency. The yield, antioxidant activities, and phytochemical contents were gradually increased as the plant grew, with the highest recorded during week 16. However, the synthesis and activities of phytochemicals were reduced in subsequent harvests despite the increment of the herbal yield. All bioactive compounds were found to be influenced insignificantly and significantly by harvesting age and harvesting frequency, respectively, specifically to shaftoside, iso-orientin, and orientin. Among all constituents, shaftoside was the main compound at various harvesting ages and harvesting frequencies. These results indicated that harvesting at week 16 with 1st harvest frequency might enhance the yield while sustaining the high synthesis of polyphenols and antioxidant activities of C. nutans.

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21

Tang, Ruotian, Chunfeng Jiang, Hongliang Li, Wei Li, and Youjun Xu. "Facile Synthesis of N-Substituted 4-Amino-6-methyl Resorcinols from Polysubstituted Cyclohexanone." Synlett 28, no. 14 (July 11, 2017): 1807–10. http://dx.doi.org/10.1055/s-0036-1590817.

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A novel synthesis of N-substituted 4-amino-6-methyl resorcinols from polysubstituted cyclohexanone was developed. The reaction was performed in an easy ‘one-pot’, tandem manner with well-tolerated substituent on the nitrogen to give the desired compound in good to excellent yield. This highly efficient method will find broad application in the synthesis of some natural products and bioactive interesting compounds.

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22

Akiba, Mitsuo, Norihiko Kakimoto, Masanao Matsui, and Toyozo Takada. "Organogermanium Compounds. Synthesis and Properties of Bioactive Germanium Sesquisulfides." HETEROCYCLES 23, no. 10 (1985): 2681. http://dx.doi.org/10.3987/r-1985-10-2681.

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23

Fukase, Koichi. "Chemical Synthesis of Bioactive Compounds: Hard Work but Enjoyable." Journal of Synthetic Organic Chemistry, Japan 80, no. 6 (June 1, 2022): 598–601. http://dx.doi.org/10.5059/yukigoseikyokaishi.80.598.

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24

Cherkasov, Rafael A., Narkis G. Khusainova, Eugeny A. Berdnikov, Mikhail A. Khusainov, and Sergey M. Rybakov. "Synthesis of Novel Bis(aminoalkenylphosphonates) as Potential Bioactive Compounds." Phosphorus, Sulfur, and Silicon and the Related Elements 186, no. 4 (March 31, 2011): 972–73. http://dx.doi.org/10.1080/10426507.2010.506666.

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25

KIYOTA, Hiromasa. "Synthesis of Naturally Derived Bioactive Compounds of Agricultural Interest." Bioscience, Biotechnology, and Biochemistry 70, no. 2 (January 2006): 317–24. http://dx.doi.org/10.1271/bbb.70.317.

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26

RESNATI, G. "ChemInform Abstract: Synthesis of Chiral and Bioactive Fluoroorganic Compounds." ChemInform 25, no. 5 (August 19, 2010): no. http://dx.doi.org/10.1002/chin.199405293.

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27

ISOBE, M. "ChemInform Abstract: Stereocontrolled Synthesis of Multi-Functional Bioactive Compounds." ChemInform 28, no. 49 (August 2, 2010): no. http://dx.doi.org/10.1002/chin.199749299.

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28

Morán, Diana, Gemma Gutiérrez, María Carmen Blanco-López, Ali Marefati, Marilyn Rayner, and María Matos. "Synthesis of Starch Nanoparticles and Their Applications for Bioactive Compound Encapsulation." Applied Sciences 11, no. 10 (May 17, 2021): 4547. http://dx.doi.org/10.3390/app11104547.

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In recent years, starch nanoparticles (SNPs) have attracted growing attention due to their unique properties as a sustainable alternative to common nanomaterials since they are natural, renewable and biodegradable. SNPs can be obtained by the breakdown of starch granules through different techniques which include both physical and chemical methods. The final properties of the SNPs are strongly influenced by the synthesis method used as well as the operational conditions, where a controlled and monodispersed size is crucial for certain bioapplications. SNPs are considered to be a good vehicle to improve the controlled release of many bioactive compounds in different research fields due to their high biocompatibility, potential functionalization, and high surface/volume ratio. Their applications are frequently found in medicine, cosmetics, biotechnology, or the food industry, among others. Both the encapsulation properties as well as the releasing processes of the bioactive compounds are highly influenced by the size of the SNPs. In this review, a general description of the different types of SNPs (whole and hollow) synthesis methods is provided as well as on different techniques for encapsulating bioactive compounds, including direct and indirect methods, with application in several fields. Starches from different botanical sources and different bioactive compounds are compared with respect to the efficacy in vitro and in vivo. Applications and future research trends on SNPs synthesis have been included and discussed.

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Khalaf, Zahraa D. "Synthesis, Spectral, Antioxidant and Antimicrobial Activity of Some New Heterocyclics containing Benzimidazole Moiety." Research Journal of Chemistry and Environment 26, no. 8 (July 25, 2022): 56–60. http://dx.doi.org/10.25303/2608rjce056060.

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Benzimidazole, as a model compound for the development of new bioactive compounds, has long been revered by organic and medicinal chemists due to unique properties of heterocyclic compounds. A comprehensive study of recent methods of synthesizing this compound will provide researchers, chemists and pharmacologists with the most up-to-date, most productive, cost-effective information possible. Benzimidazole compounds might be important in developing novel medications in the future because of their speedy, easy, efficient and environmentally friendly production, characterization and biological investigation. FTIR and 1HNMR data for the spectroscopic characterization; compared to BHT demonstrated significant antioxidant and antibacterial activity.

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Tarko, T., A. Duda-Chodak, and M. Kobus. "Influence of growth medium composition on synthesis of bioactive compounds and antioxidant properties of selected strains of Arthrospira cyanobacteria." Czech Journal of Food Sciences 30, No. 3 (April 27, 2012): 258–67. http://dx.doi.org/10.17221/46/2011-cjfs.

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We studied how the selection of the growth medium influences the antioxidant properties and synthesis of bioactive compounds (β-carotene, C-phycocyanin, allophycocyanin, and phycoerythrin) in six selected species of cyanobacteria of Arthrospira genus. For this purpose, cyanobacteria cultures were cultivated on a typical Zarrouk medium and on a cheaper substitute – RM6 medium. Significant differences were observed in the efficiency of synthesis of the studied compounds depending on the strain of cyanobacteria. The quantitative and qualitative composition of Zarrouk medium was more beneficial for β-carotene synthesis in the cells of all strains of cyanobacteria studied. This medium also allowed for the antioxidant potential of the studied strains to be increased. On the other hand, the RM6 medium, deprived of some mineral ingredients, enabled more efficient synthesis of phycobiliproteins in all studied strains except A. platensis SAG 85.79.  

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Li, Tingting, Ting Ding, and Jianrong Li. "Medicinal Purposes: Bioactive Metabolites from Marine-derived Organisms." Mini-Reviews in Medicinal Chemistry 19, no. 2 (December 6, 2018): 138–64. http://dx.doi.org/10.2174/1389557517666170927113143.

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The environment of marine occupies about 95% biosphere of the world and it can be a critical source of bioactive compounds for humans to be explored. Special environment such as high salt, high pressure, low temperature, low nutrition and no light, etc. has made the production of bioactive substances different from terrestrial organisms. Natural ingredients secreted by marine-derived bacteria, fungi, actinomycetes, Cyanobacteria and other organisms have been separated as active pharmacophore. A number of evidences have demonstrated that bioactive ingredients isolated from marine organisms can be other means to discover novel medicines, since enormous natural compounds from marine environment were specified to be anticancer, antibacterial, antifungal, antitumor, cytotoxic, cytostatic, anti-inflammatory, antiviral agents, etc. Although considerable progress is being made within the field of chemical synthesis and engineering biosynthesis of bioactive compounds, marine environment still remains the richest and the most diverse sources for new drugs. This paper reviewed the natural compounds discovered recently from metabolites of marine organisms, which possess distinct chemical structures that may form the basis for the synthesis of new drugs to combat resistant pathogens of human life. With developing sciences and technologies, marine-derived bioactive compounds are still being found, showing the hope of solving the problems of human survival and sustainable development of resources and environment.

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Vágvölgyi, Máté, Endre Kocsis, Márta Nové, Nikoletta Szemerédi, Gabriella Spengler, Zoltán Kele, Róbert Berkecz, Tamás Gáti, Gábor Tóth, and Attila Hunyadi. "Diversity-Oriented Synthesis Catalyzed by Diethylaminosulfur-Trifluoride—Preparation of New Antitumor Ecdysteroid Derivatives." International Journal of Molecular Sciences 23, no. 7 (March 22, 2022): 3447. http://dx.doi.org/10.3390/ijms23073447.

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Fluorine represents a privileged building block in pharmaceutical chemistry. Diethylaminosulfur-trifluoride (DAST) is a reagent commonly used for replacement of alcoholic hydroxyl groups with fluorine and is also known to catalyze water elimination and cyclic Beckmann-rearrangement type reactions. In this work we aimed to use DAST for diversity-oriented semisynthetic transformation of natural products bearing multiple hydroxyl groups to prepare new bioactive compounds. Four ecdysteroids, including a new constituent of Cyanotis arachnoidea, were selected as starting materials for DAST-catalyzed transformations. The newly prepared compounds represented combinations of various structural changes DAST was known to catalyze, and a unique cyclopropane ring closure that was found for the first time. Several compounds demonstrated in vitro antitumor properties. A new 17-N-acetylecdysteroid (13) exerted potent antiproliferative activity and no cytotoxicity on drug susceptible and multi-drug resistant mouse T-cell lymphoma cells. Further, compound 13 acted in significant synergism with doxorubicin without detectable direct ABCB1 inhibition. Our results demonstrate that DAST is a versatile tool for diversity-oriented synthesis to expand chemical space towards new bioactive compounds.

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33

İ MAHMOOD, Israa, Salih SALMAN, and Luma ABD. "New Bioactive Aromatic Heterocyclic Macromolecules with Monosaccharide Core." Journal of the Turkish Chemical Society Section A: Chemistry 9, no. 3 (August 31, 2022): 889–900. http://dx.doi.org/10.18596/jotcsa.1098055.

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1,1,2-trimethyl-1H-benzo[e]indole is an important heterocyclic compound, its available in reasonable price and can easily modified to make a good intermediate for other derivatives. That is quite enough reasons to use as starting material for a new series of compounds with other biomolecules such as monosaccharides after simple modification. The target molecules show biological activity. So, the current work is aiming to improve the activity and the properties of the benzo indole by attaching with a naturally occurring, and biodegradable compounds represented by 2-deoxy-2-amino -d-glucose and 6-deoxy-6-amino-d-glucose to synthesis both mono and di-saccharides derivatives of benzo indole. Two steps synthesis were used for mono-saccharide derivatives and three steps for di-saccharide derivatives, the first is the functionalization of 1,1,2-trimethyl-1H-benzo[e]indole [1] via the reaction with POCl3 to produce 2-(1,1-dimethyl-1H-benzo[e]indol-2(3H)-ylidene) malonaldehyde [2] with two aldehydes reaction centers, while in the second step the latter was coupled with sugar via amino groups to get the two monosaccharide derivatives [3,5], while the disaccharides molecules [4,6] taken one more step with harder conditions to overcome the steric hindrance at the other reaction center. The purity and characterization of the target molecules was confirmed using spectroscopy methods including 1H NMR and 13 NMR. The synthesized compound shows a good biological activity as antibacterial antifungal.

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Tarigan, Indra Lasmana, Ayu Kumala Sari, Choirul Huda, Czellicya Jovanncha, and Afidatul Muadifah. "Phytochemical Screening and Quantitative Analysis of Coleus arthropurpureus Ethyl Acetate Fraction and Antibacterial Activity Against Staphylococcus aureus." ALKIMIA : Jurnal Ilmu Kimia dan Terapan 4, no. 1 (February 29, 2020): 17–23. http://dx.doi.org/10.19109/alkimia.v4i1.5123.

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Staphylococcus aureus (S. aureus) is a pathogenic microbe that is caused by various diseases in humans and animals. Infectious diseases caused by S. aureus in Asia reached 70% in 2007, while in Indonesia reached 23.5%. The plant provided several bioactive compounds that might function as an antibacterial which inhibits both bacterial growth and damaging the cell system and protein synthesis. Coleus arthropurpureus known contains alkaloids and tannins that supposed to be an antibacterial compound. Tannins have antibacterial activity, in general, the mechanism is to damage the bacterial cell membrane and induce the formation of complex compound bonds to enzymes or microbial substrates. This study aims to analyze the bioactive compounds contained in C. arthropurpureus in qualitative and quantitative which have an antimicrobial function using high-performance liquid chromatography (HPLC) in the reverse phase C-18 column and screening of antibacterial activity was carried out by disc diffusion method. The results of both qualitative and quantitative analysis by HPLC has obtained the presence of tannin bioactive compounds (1.48 ppm at a retention time of 2.806 minutes) and alkaloids (1.11 ppm at a retention time of 7.015). Moreover, we verified the diameter of inhibition of growth zone against S. aureus at a concentration of 15% extract was 12.80 mm. It was found that the highest percentage of the bioactive compound in C. arthropurpureus is tannin, and that is might an antibacterial agent.

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Tiwari, Abhitav, Shambhawi Pritam, Keerti Mishra, Mehshara Khan, Neeraj Upmanyu, and Dipanjana Ghosh. "Nutraceuticals from Marine Bionetworks." Current Nutrition & Food Science 15, no. 4 (June 28, 2019): 338–44. http://dx.doi.org/10.2174/1573401314666180109153825.

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“Nutrition” and “Pharmaceutical” together build up the perception of “Nutraceuticals” that refer to the food or dietary supplements that help to incorporate additional health benefits to the fundamental sustenance accomplished on daily basis. Each nutraceutical contains one or more bioactive molecules that are usually obtained by chemical and/ or biotechnological synthesis or by extraction from natural sources. Among the natural sources, marine bionetwork possess immense potential for the presence of bioactive compounds. Some of these bioactive compounds as isolated from marine sources, have potential use as nutraceuticals. This mini review provides a brief overview of nutraceutical compounds from marine sources that are currently under research and/or have been commercialized. A detailed discussion on the biochemical categories of compounds and the marine organisms that play as potential sources of these bioactive nutraceutical compounds have been included.

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Martínková, Ludmila, Barbora Křístková, and Vladimír Křen. "Laccases and Tyrosinases in Organic Synthesis." International Journal of Molecular Sciences 23, no. 7 (March 22, 2022): 3462. http://dx.doi.org/10.3390/ijms23073462.

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Laccases (Lac) and tyrosinases (TYR) are mild oxidants with a great potential in research and industry. In this work, we review recent advances in their use in organic synthesis. We summarize recent examples of Lac-catalyzed oxidation, homocoupling and heterocoupling, and TYR-catalyzed ortho-hydroxylation of phenols. We highlight the combination of Lac and TYR with other enzymes or chemical catalysts. We also point out the biological and pharmaceutical potential of the products, such as dimers of piceid, lignols, isorhamnetin, rutin, caffeic acid, 4-hydroxychalcones, thiols, hybrid antibiotics, benzimidazoles, benzothiazoles, pyrimidine derivatives, hydroxytyrosols, alkylcatechols, halocatechols, or dihydrocaffeoyl esters, etc. These products include radical scavengers; antibacterial, antiviral, and antitumor compounds; and building blocks for bioactive compounds and drugs. We summarize the available enzyme sources and discuss the scalability of their use in organic synthesis. In conclusion, we assume that the intensive use of laccases and tyrosinases in organic synthesis will yield new bioactive compounds and, in the long-term, reduce the environmental impact of industrial organic chemistry.

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Sugai, Takeshi. "Biochemical Asymmetric Synthesis and Its Application to Chemical Synthesis of Bioactive Compounds." Journal of the agricultural chemical society of Japan 69, no. 1 (1995): 9–16. http://dx.doi.org/10.1271/nogeikagaku1924.69.9.

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Polshettiwar, Vivek, and Rajender S. Varma. "Greener and expeditious synthesis of bioactive heterocycles using microwave irradiation." Pure and Applied Chemistry 80, no. 4 (January 1, 2008): 777–90. http://dx.doi.org/10.1351/pac200880040777.

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The utilization of green chemistry techniques is dramatically reducing chemical waste and reaction times as has recently been proven in several organic syntheses and chemical transformations. To illustrate these advantages in the synthesis of bioactive heterocycles, we have studied various environmentally benign protocols that involve greener alternatives. Microwave (MW) irradiation of neat reactants catalyzed by the surfaces of recyclable mineral supports, such as alumina, silica, clay, or their "doped" versions, enables the rapid one-pot assembly of heterocyclic compounds, such as flavonoids, related benzopyrans, and quinolone derivatives. The strategy to assemble oxygen and nitrogen heterocycles from in situ generated reactive intermediates via enamines or using hypervalent iodine reagents is described. Examples of multicomponent reactions that can be adapted for rapid parallel synthesis include solventless synthesis of dihydropyrimidine-2(1H)-ones (Biginelli reaction), imidazo[1,2-a]annulated pyridines, pyrazines, and pyrimidines (Ugi reaction). The relative advantages of greener pathways, which use MW irradiation and eco-friendly aqueous reaction medium, for the synthesis of various heterocycles, such as N-aryl azacycloalkanes, isoindoles, 1,3-dioxane, 1,3,4-oxadiazole, 1,3,4-thiadiazole, pyrazole, and diazepines, are also summarized.

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Pellissier, Hélène. "Asymmetric Organocatalytic Tandem/Domino Reactions to Access Bioactive Products." Current Organic Chemistry 25, no. 13 (September 2, 2021): 1457–71. http://dx.doi.org/10.2174/1385272825666210208142427.

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Tandem and domino reactions constitute economic methodologies to prepare complex molecules starting from simple materials. Especially, combining these powerful procedures to asymmetric catalysis allows direct access to many elaborated chiral products, including important key intermediates in total syntheses of important biologically active compounds. A range of various types of chiral organocatalysts have already been successfully applied to such syntheses. This review presents major developments in the total synthesis of bioactive products based on the use of enantioselective organocatalytic domino/tandem reactions as key steps. It is divided into three parts, dealing successively with syntheses based on organocatalytic asymmetric Michael-initiated domino reactions as key steps; aldol-initiated domino/tandem reactions and other domino reactions.

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Goetzke, F. Wieland, Mireia Sidera, and Stephen P. Fletcher. "Catalytic asymmetric hydrometallation of cyclobutenes with salicylaldehydes." Chemical Science 13, no. 1 (2022): 236–40. http://dx.doi.org/10.1039/d1sc06035j.

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Hardiningtyas, Safrina Dyah, Febby Amanda Putri, and Iriani Setyaningsih. "Antibacterial activity of ethanolic Spirulina platensis extract-water soluble chitosan nanoparticles." IOP Conference Series: Earth and Environmental Science 1033, no. 1 (June 1, 2022): 012053. http://dx.doi.org/10.1088/1755-1315/1033/1/012053.

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Abstract Spirulina platensis is a microalga containing bioactive compound as antibacterial activity. The antibacterial compound from Spirulina can be used to treat bacterial infections on the skin such as acne. However, enhancement penetration of bioactive compounds through the skin was needed. The objective of this study was to determine bioactive compounds from Spirulina, synthesize Spirulina extract-water soluble chitosan nanoparticles using the ionic gelation method, and measure the antibacterial activity of Spirulina extract and its nanoparticles. For the synthesis of the nanoparticles, differences of Spirulina extract concentrations were used, including 3.25, 7.5, and 15 mg/mL. The yield of ethanolic Spirulina extract was 13.87±4.16% with the bioactive components of saponins, tannins, steroids, and phenols. The Spirulina extract-loaded chitosan nanoparticles were successfully fabricated with a nano-range size and narrow polydispersity. The amount of loading of Spirulina extract has affected the size and dispersion of nanoparticles. The antibacterial activity of nanoparticles showed higher than pure Spirulina extract only through Staphylococcus aureus and Pseudomonas aeruginosa, classified as moderate inhibition zones (5-10 mm). These suggested that nanoencapsulation could increase extract uptake on bacteria cells. The ethanolic Spirulina extract-chitosan nanoparticles have a potency for antibacterial agents on cosmeceutical products.

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Erenler, Ramazan, and Esma Nur Geçer. "Green synthesis of silver nanoparticles from Astragalus logopodioides L. leaves." Turkish Journal of Agriculture - Food Science and Technology 10, no. 6 (July 3, 2022): 1112–15. http://dx.doi.org/10.24925/turjaf.v10i6.1112-1115.5190.

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Natural products have gained great interest due to their broad spectrum of biological activities and bioactive compounds. In this study, silver nanoparticles (AgNPs) were synthesized using Astragalus logopodioides L. by green approach. The structure of AgNPs was elucidated by spectroscopic techniques. UV-Vis spectrum presented the maximum absorption of AgNPs as 419 nm. The crystal structure of AgNPs was assigned as face centered cubic by X-ray diffraction (XRD) pattern. Scanning electron microscope (SEM) established morphology of AgNPs with an average size of 36.4 nm. A. logopodioides included the bioactive compounds, So, AgNPs capped by these compounds could be valuable substances for food and pharmaceutical applications.

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43

Karaburun, Ahmet, Ulviye Acar Çevik, Derya Osmaniye, Begüm Sağlık, Betül Kaya Çavuşoğlu, Serkan Levent, Yusuf Özkay, Ali Koparal, Mustafa Behçet, and Zafer Kaplancıklı. "Synthesis and Evaluation of New 1,3,4-Thiadiazole Derivatives as Potent Antifungal Agents." Molecules 23, no. 12 (November 29, 2018): 3129. http://dx.doi.org/10.3390/molecules23123129.

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With the goal of obtaining a novel bioactive compound with significant antifungal activity, a series of 1,3,4-thiadiazole derivatives (3a–3l) were synthesized and characterized. Due to thione-thiol tautomerism in the intermediate compound 2, type of substitution reaction in the final step was determined by two-dimensional (2D) NMR. In vitro antifungal activity of the synthesized compounds was evaluated against eight Candida species. The active compounds 3k and 3l displayed very notable antifungal effects. The probable mechanisms of action of active compounds were investigated using an ergosterol quantification assay. Docking studies on 14-α-sterol demethylase enzyme were also performed to investigate the inhibition potency of compounds on ergosterol biosynthesis. Theoretical absorption, distribution, metabolism, and excretion (ADME) predictions were calculated to seek their drug likeness of final compounds. The results of the antifungal activity test, ergosterol biosynthesis assay, docking study, and ADME predictions indicated that the synthesized compounds are potential antifungal agents, which inhibit ergosterol biosynthesis probably interacting with the fungal 14-α-sterol demethylase.

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Gemechu, Warkina. "Review on Changes in Bioactive Composition of Fruits during Juice Processing." Food Science & Nutrition Technology 5, no. 5 (September 30, 2020): 1–9. http://dx.doi.org/10.23880/fsnt-16000230.

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Fruits and vegetables are consumed at all times, and due to their convenient size; they are an excellent between-meal snack. Fruit juices are naturally rich in bioactive compositions like phenolic compounds. However, in some other cases heat processing may partially destroy them or significantly reduce their bioavailability, thus reducing beneficial health effects. Modern processing, packaging, ingredient technology and distribution systems are taken as a system that assure safe, stable and appealing fruit juice products in a convenient, economical form far from the raw material source or season. Fruits may contain different bioactive compounds, many of which may have antioxidant capacity. Many complex biochemical reactions are involved during the ripening process, such as the hydrolysis of starch and the synthesis of carotenoids, anthocyanins, and phenolic compounds in addition to the formation of various volatile compounds. The processing such as thermal pasteurization and sterilization, pulsed electric fields, high pressure, ultrasound, microwave treatment, and microfiltration aimed to preserve fruit juices due to their ability to inactivate a wide range of microorganism’s and spoilage enzymes may have another effect on bioactive compounds. So that avoiding over processing to save bioactive nutrients and following the best juice processing methods, adopting high energy transfer processing method such as high temperature short time pasteurization to reduce the treatment time, improving temperature and time combination in processing is recommended.

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Mikołajczyk, Marian. "Phosphonate reagents and building blocks in the synthesis of bioactive compounds, natural products and medicines." Pure and Applied Chemistry 91, no. 5 (May 27, 2019): 811–38. http://dx.doi.org/10.1515/pac-2018-1117.

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Abstract This account outlines the results obtained in the author’s laboratory on the application of phosphonates in the synthesis of various classes of biologically active cyclopentenones and cyclopentanones. In the first place two general methods for the synthesis of mono-, 1,2- and 1,4-dicarbonyl compounds are presented. The first is based on the use of α-phosphoryl sulfides in conjunction with the Horner reaction while in the second method the oxygenation reaction of α-phosphonate carbanion is a key step. The utility of these two approaches to 1,4-diketones as precursors of cyclopentenones was exemplified by the synthesis of dihydrojasmone and (Z)-jasmone. The use of simple phosphonates, α-phosphoryl sulfides and β- and γ-ketophosphonates as starting reagents in the synthesis of cyclopentanoid antibiotics (methylenomycin B, racemic desepoxy-4,5-didehydromethylenomycin, enantiomeric sarkomycins) is presented. The synthesis and reactivity of achiral 3-(phosphorylmethyl)cyclopent-2-enone and chiral diastereoisomeric camphor protected 3-(phosphorylmethyl)-4,5-dihydroxycyclopent-2-enones as building blocks is discussed as a platform for developing a new access to a variety of bioactive cyclopentenones. The utility and value of achiral phosphonate building block is demonstrated by the synthesis of racemic and enantiopure prostaglandin B1 methyl esters and enantiomeric phytoprostanes B1 type I and II. The range of biologically active compounds prepared from chiral diastereoisomeric cyclopentenone phosphonates is wider. Herein the total syntheses of the following target compounds are presented: enantiomeric isoterreins, natural (−)-neplanocin A and its unnatural (+)-enantiomer, anticancer prostaglandin analogues (enantiomers of TEI-9826, NEPP-11, iso-NEPP-11). The design and synthesis of racemic and four enantiopure stereoisomers of an antiulcer drug rosaprostol is also described.

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Jindal, Rani, and Sanjay Bajaj. "Recent Applications of Microwaves in Synthesis of Bioactive Heterocyclic Compounds." Current Organic Chemistry 12, no. 10 (July 1, 2008): 836–49. http://dx.doi.org/10.2174/138527208784911842.

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N. Sangshetti, Jaiprakash, Abhay S. Zambare, Indrajeet Gonjari, and Devanand B. Shinde. "Pfitzinger Reaction in the Synthesis of Bioactive Compounds - A Review." Mini-Reviews in Organic Chemistry 11, no. 2 (June 2014): 225–50. http://dx.doi.org/10.2174/1570193x113106660020.

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Hayes, Patricia Y., Sharon Chow, Fredrik Rahm, Paul V. Bernhardt, James J. De Voss, and William Kitching. "Synthesis of the Sponge-Derived Plakortone Series of Bioactive Compounds." Journal of Organic Chemistry 75, no. 19 (October 2010): 6489–501. http://dx.doi.org/10.1021/jo101224w.

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TACHIBANA, Yoji. "Synthesis and Structure-Activity Relationships of Bioactive Compounds Using Sterols." YAKUGAKU ZASSHI 126, no. 11 (November 1, 2006): 1139–54. http://dx.doi.org/10.1248/yakushi.126.1139.

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Ferreira, Marco, Luiz Dias, Ives Leonarczyk, Ellen Polo, and Emílio de Lucca. "Exploring the Aldol Reaction in the Synthesis of Bioactive Compounds." Current Organic Synthesis 12, no. 5 (August 21, 2015): 547–64. http://dx.doi.org/10.2174/157017941205150821124901.

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