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Journal articles on the topic 'Compound with biological activities'

Author: Grafiati

Published: 4 June 2021

Last updated: 17 February 2022

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1

Rode, Milind, Sahebrao Rindhe, and Bhausaheb Karale. "Synthesis and biological activities of some indoline derivatives." Journal of the Serbian Chemical Society 74, no. 12 (2009): 1377–87. http://dx.doi.org/10.2298/jsc0912377r.

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The reaction of indoline with a substituted benzoyl chloride in the presence of K2CO3 in THF gave compound 4. Compound 4 was subjected to chlorosulphonation to obtain compound 5. Condensation of aromatic amines with compound 5 led to the synthesis of indoline derivatives 6(a-f). Similarly, 5-nitroindoline was treated with a substituted benzoyl chloride to obtain the nitro compound 9, which was reduced using stannous chloride and reacted further with aromatic sulphonyl chloride to obtain the indoline derivatives 11(a-e). These compounds were tested for antibacterial, anti-tuberculosis and antif

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2

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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3

Verma, Amita, Sunil Joshi, and Deepika Singh. "Imidazole: Having Versatile Biological Activities." Journal of Chemistry 2013 (2013): 1–12. http://dx.doi.org/10.1155/2013/329412.

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Imidazoles have occupied a unique position in heterocyclic chemistry, and its derivatives have attracted considerable interests in recent years for their versatile properties in chemistry and pharmacology. Imidazole is nitrogen-containing heterocyclic ring which possesses biological and pharmaceutical importance. Thus, imidazole compounds have been an interesting source for researchers for more than a century. The imidazole ring is a constituent of several important natural products, including purine, histamine, histidine, and nucleic acid. Being a polar and ionisable aromatic compound, it imp

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4

Lu, Jie, Jing Tian, Li Zhou, et al. "Phytochemistry and Biological Activities of Poria." Journal of Chemistry 2021 (March 29, 2021): 1–20. http://dx.doi.org/10.1155/2021/6659775.

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Poria is a common Traditional Chinese Medicine in clinic. In recent years, the chemical and pharmacological studies of Poria have made great progress, triterpenes and polysaccharides have been isolated, and various types of compounds containing lipids, octanoic acids, fatty acids, and trace elements have been found. In this paper, we reviewed the literature, summarized the main compound types, and reviewed in detail their pharmacological effects in antitumor, immunomodulatory, effects on kidney, hepatoprotective activity, effects on blood sugar, antioxidant effects, anti-inflammatory effects,

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5

Ngoc, Thuc Dinh, Wim Dehaen, Luc Van Meervelt, and Jan Balzarini. "Synthesis of Heterocyclic Triterpene Derivatives with Biological Activities via Click Reaction." Current Organic Chemistry 23, no. 26 (2020): 2969–74. http://dx.doi.org/10.2174/1385272823666191212110411.

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: Grignard reactions were applied to synthesize 2-ethynyl-2-hydroxylallobetulin 5 from 2-oxoallobetulin 4. The compound plays an important role as starting material to synthesize heterocyclic triterpenes using the click reaction. A series of new 1,2,3-triazole derivatives derived from 2-oxoallobetulin were successfully obtained. Under similar reaction conditions, only one compound 6 kept the hydroxyl functional group, while in the other compounds 7, 8 and 9, water was eliminated. The structures of obtained compounds were confirmed by 2D-NMR spectroscopy. The X-ray analysis of 5 indicated that

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6

San, Htoo Tint, Tanawat Chaowasku, Wanwimon Mekboonsonglarp, et al. "Constituents of Huberantha jenkinsii and Their Biological Activities." Molecules 25, no. 15 (2020): 3533. http://dx.doi.org/10.3390/molecules25153533.

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The phytochemical investigation of Huberantha jenkinsii resulted in the isolation of two new and five known compounds. The new compounds were characterized as undescribed 8-oxoprotoberberine alkaloids and named huberanthines A and B, whereas the known compounds were identified as allantoin, oxylopinine, N-trans-feruloyl tyramine, N-trans-p-coumaroyl tyramine, and mangiferin. The structure determination was accomplished by spectroscopic methods. To evaluate therapeutic potential in diabetes and Parkinson’s disease, the isolates were subjected to assays for their α-glucosidase inhibitory activit

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7

HERNAWAN, UDHI EKO, and AHMAD DWI SETYAWAN. "REVIEW: Ellagitannin; biosynthesis, isolation, and biological activities." Biofarmasi Journal of Natural Product Biochemistry 1, no. 1 (2003): 25–38. http://dx.doi.org/10.13057/biofar/f010105.

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Ellagitannin is one of the bioactive groups produced by some of medicinal plants. Ellagitannin is a hydrolysable tannin compound biosynthesized via shikimic acid â€“ gallic acid â€“ pentagalloilglucose pathway. Ellagitannin can be isolated by cascade extraction procedures followed by column chromatography method and preparative HPLC method. The biological activities of ellagitannin are caused by molecular bond between ellagitannin and some other compound, especially protein that makes complex compound and changes physiological processes in cells or tissues of the livingthinks. Biological activ

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8

SHIMOMURA, Toru, and Yuko OHASHI. "Biological activities of organogermanium compound, an interferon inducer." Japanese Journal of Phytopathology 52, no. 5 (1986): 865–69. http://dx.doi.org/10.3186/jjphytopath.52.865.

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9

Yang, Jian, Yongtian Zhao, Jun Wan, et al. "Synthesis and Biological Evaluation of Novel Benodanil-Heterocyclic Carboxamide Hybrids as a Potential Succinate Dehydrogenase Inhibitors." Molecules 25, no. 18 (2020): 4291. http://dx.doi.org/10.3390/molecules25184291.

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In order to discover new antifungal agents, twenty novel benodanil-heterocyclic carboxamide hybrids were designed, synthesized, and characterized by 1H NMR and HRMS. In vitro, their antifungal activities against four phytopathogenic fungi were evaluated, as well as some of the target compounds at 50 mg/L demonstrated significant antifungal activities against Rhizoctonia solani. Especially, compounds 17 (EC50 = 6.32 mg/L) and 18 (EC50 = 6.06 mg/L) exhibited good antifungal activities against R. solani and were superior to the lead fungicide benodanil (a succinate dehydrogenase inhibitor, SDHI)

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10

Manjula, J., and R. Maheswari. "BIOLOGICAL AND DOCKING STUDIES OF NOVEL AROYLHYDRAZONES." International Journal of Pharmacy and Pharmaceutical Sciences 9, no. 5 (2017): 81. http://dx.doi.org/10.22159/ijpps.2017v9i5.10862.

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Objective: Novel aroylhydrazone schiff bases were synthesized and were screened for their biological activities.Methods: Using HCl as a catalyst, all the compounds were synthesized at room temperature and were characterized by IR and NMR techniques. The synthesized Schiff bases were screened for antibacterial, antifungal activities. In silico molecular docking, method was performed to study their anti-tuberculosis activity against enoyl acyl carrier protein reductase (InhA) from Mycobacterium tuberculosis (PDB id: 2NSD). Results: Compound P1 showed good antibacterial activity against gram posi

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11

Yang, Sen, Xiao-Yu Tian, Tian-Yang Ma, et al. "Synthesis and Biological Activity of Benzamides Substituted with Pyridine-Linked 1,2,4-Oxadiazole." Molecules 25, no. 15 (2020): 3500. http://dx.doi.org/10.3390/molecules25153500.

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To find pesticidal lead compounds with high activity, a series of novel benzamides substituted with pyridine-linked 1,2,4-oxadiazole were designed by bioisosterism, and synthesized easily via esterification, cyanation, cyclization and aminolysis reactions. The structures of the target compounds were confirmed by 1H-NMR, 13C-NMR and HRMS. The preliminary bioassay showed that most compounds had good larvicidal activities against mosquito larvae at 10 mg/L, especially compound 7a, with a larvicidal activity as high as 100%, and even at 1 mg/L was still 40%; at 50 mg/L, all the target compounds sh

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12

Lin, Gui-Shan, Chang-Hua Ma, Wen-Gui Duan, Bo Cen, Fu-Hou Lei та Zhang-Qi Yang. "Synthesis and biological activities of α-pinene-based dithiadiazoles". Holzforschung 68, № 1 (2014): 75–83. http://dx.doi.org/10.1515/hf-2013-0006.

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Abstract This work is aiming at the preparation of new bioactive compounds from α-pinene as starting material. To this purpose, the intermediates (disubstituted phenyl acylamino thioureas, class G) were cyclized to dithiadiazoles (class H). The intermediates and target compounds were analyzed by Fourier transform infrared, 1H nuclear magnetic resonance (NMR), 13C NMR, and electrospray ionization-mass spectrometry and elemental analysis. The bioassay experiments showed that the compounds G and H have herbicidal, fungicidal, and plant growth-regulating activities. The compounds 2,2′-dimethylphen

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13

Akramov, Davlat Kh, Nilufar Z. Mamadalieva, Andrea Porzel, et al. "Sugar Containing Compounds and Biological Activities of Lagochilus setulosus." Molecules 26, no. 6 (2021): 1755. http://dx.doi.org/10.3390/molecules26061755.

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Phytochemical investigation of the methanolic extract obtained from the aerial parts of Lagochilus setulosus (Lamiaceae) afforded the new compound 1-methoxy-3-O-β-glucopyranosyl-α-l-oliose (1) together with five known glycosides, namely sitosterol-3-O-β-glucoside (2), stigmasterol-3-O-β-glucoside (3), pinitol (4), 6β-hydroxyl-7-epi-loganin (5), and chlorotuberoside (6). The structures of these compounds were elucidated by extensive spectroscopic analyses, especially HR-MS, 1D and 2D NMR spectroscopy. The in vitro cytotoxic activity of the methanolic extract and the isolated compounds was asses

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14

Zhang, Mingqian, Binkai Liu, Qiang Lei, Jingdong Yan, Zhongyu Zhao, and Yue Long. "Synthesis and Biological Activities of 1,3,4-Thiadiazole Triazene Compound." Chinese Journal of Organic Chemistry 39, no. 4 (2019): 1064. http://dx.doi.org/10.6023/cjoc201809003.

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15

Mohammed, Hamid H., Zaizafoone N. Nasif, Zainab N. Mageed, and S. Ahmed. "Synthesis and Biological Activities of New Fused Pyrimidine Compound." Asian Journal of Chemistry 30, no. 3 (2018): 661–66. http://dx.doi.org/10.14233/ajchem.2018.21093.

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16

Peter Osarodion Osarumwense, Mary Olire Edema, and Cyril Odianosen Usifoh. "Synthesis and antibacterial activities of quinazolin-4(3h)-one, 2-methyl-4(3h)-quinazolinone and 2–phenyl-4(3h)-quinazolinone." International Journal of Biological and Pharmaceutical Sciences Archive 1, no. 2 (2021): 077–84. http://dx.doi.org/10.30574/ijbpsa.2021.1.2.0027.

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Background: Quinazoline and quinazolinone scaffolds represent an important class of biologically active nitrogen heterocyclic compounds. Many marketed drugs are based on these moieties. A diverse range of molecules with quinazoline/quinazolinone moieties have been reported to exhibit broad spectrum of biological activities Objective: This study is aimed at the synthesis of these quinazolinone derivatives, quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one and evaluate them for their antibacterial activities. Method: The consolidation of 2-amino-methyl-4-

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17

Khani-Meinagh, Hossein, Hossein Mostafavi, and Majid Mahdavi. "Synthesis and Biological Evaluation of Some Novel 2-Pyrazinoic Acidderived Esters." Letters in Organic Chemistry 16, no. 5 (2019): 424–29. http://dx.doi.org/10.2174/1570178615666180806122226.

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Pyrazine, a kojic acid having hydroxypyrone, and hydroquinone are the head compounds of different categories possessing a broad range of biological activities including anticancer and antioxidant activities, thus are interested in evaluating the cytotoxicity on K562 human leukemia cells and radical scavenging activities of these compounds in bonding together as ester compounds. Four hydroxypyrone containing-2-pyrazinoic esters along with hydroquinone containing-one were synthesized and characterized by spectral data. The cytotoxicity of these compounds on K562 human leukemia cells and free Rad

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18

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 (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.

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19

Yang, Ying, Wen-Jun Mao, Huan-Qiu Li, et al. "Synthesis and Biological Evaluation of 7-O-Modified Formononetin Derivatives." Research Letters in Organic Chemistry 2008 (December 18, 2008): 1–4. http://dx.doi.org/10.1155/2008/209830.

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Three series of novel formononetin derivatives were synthesized, in which formononetin and heterocyclic moieties were separated by 2-carbon, 3-carbon, and 4-carbon spacers. The chemical structures of these compounds were confirmed. All the derivatives were screened for antiproliferative activities against Jurkat cell line and HepG-2 cell line. In this paper, compounds prepared were also screened for their antibacterial activity of six bacterial strains. Compound 3b exihibited promising antibacterial activity against B. subtilis with minimal inhibitory concentration (MIC) value of 0.78 μg/mL, a

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20

Laddha, Purushottam R., and Kailash R. Biyani. "Synthesis and Biological Evaluation of Novel Schiff Bases of Aryloxy Moiety." Journal of Drug Delivery and Therapeutics 9, no. 5-s (2019): 44–49. http://dx.doi.org/10.22270/jddt.v9i5-s.3635.

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Schiff's bases are condensation products of primary amines with carbonyl compounds. Schiff bases (imines) possess wide variety of biological activities that include antibacterial and antifungal activity. In present work, Schiff bases from 3,5- Dimethoxyphenol (aryloxy moiety) as starting material synthesized. Esterification of 3,5- Dimethoxyphenol led to formation of (3,5-Dimethoxy-phenoxy)-acetic acid ethyl ester (1). (3,5-Dimethoxy-phenoxy)-acetic acid hydrazide (2) is derived from Compound (1) by hydrazination. Compound (2) was reacted with different aromatic aldehydes to yield novel imines

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21

Gupta, Jeetendra Kumar, and Pradeep Mishra. "ANTIMICROBIAL AND ANTHELMINTIC ACTIVITIES OF SOME NEWLY SYNTHESIZED TRIAZOLES." Asian Journal of Pharmaceutical and Clinical Research 10, no. 6 (2017): 139. http://dx.doi.org/10.22159/ajpcr.2017.v10i6.17800.

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Objective: The objective of this work is to synthesize and evaluate some novel 1,2,4-triazoles.Methods: Procedure includes synthesis of triazole compounds followed by biological evaluations. The synthesis was carried out in six steps withp-bromobenzoic acid as starting material and converting to ester and then to hydrazide. Hydrazide was then converted to 4-amino triazole. Theamino triazole was then linked to different secondary amines using chloroacetyl chloride as the linking agent. All the synthesized compounds werecharacterized through Fourier transform infrared spectroscopy, gas chromatog

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22

Khan, Hamayun, Hazrat Amin, Asad Ullah, et al. "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 compa

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23

Gomaa Darwish, Ahmed Gomaa, Mamdouh Nabil Samy, Sachiko Sugimoto, Hideaki Otsuka, and Katsuyoshi Matsunami. "A New Macrolactone, Racemolide Along With Seven Known Compounds With Biological Activities From Mangrove Plant,Lumnitzera racemosa." Natural Product Communications 14, no. 6 (2019): 1934578X1986125. http://dx.doi.org/10.1177/1934578x19861255.

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One new macrolide, racemolide (1), was isolated from an MeOH extract of the leaves of Lumnitzera racemosa with 7 known compounds (2-8) by various chromatographic techniques via silica gel, octadecylsilyl column chromatography and high-performance liquid chromatography. The structure of the new compound was determined through a combination of spectroscopic and chemical analyses. The isolated compounds were evaluated for their antileishmanial, hepatoprotective, and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities. Compound 1 showed potent antileishmanial activity at inhibition

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24

Ikhtiarudin, Ihsan, Nesa Agistia, Neni Frimayanti, Tria Harlianti, and Jasril Jasril. "Microwave-assisted synthesis of 1-(4-hydroxyphenyl)-3-(4-methoxyphenyl)prop-2-en-1-one and its activities as an antioxidant, sunscreen, and antibacterial." Jurnal Kimia Sains dan Aplikasi 23, no. 2 (2020): 51–60. http://dx.doi.org/10.14710/jksa.23.2.51-60.

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Chalcone analogs have been reported to have a variety of exciting biological activities, such as anticancer, anti-inflammatory, antioxidant, photoprotective, antibacterial, and antidiabetic activities. Therefore, analogs of these compounds have been widely synthesized as intermediate compounds or target molecules in the discovery of bioactive compounds to be applied in the pharmaceutical field. The purpose of this study is to synthesize chalcone analog compounds (E)-1-(4-hydroxyphenyl)-3-(4-methoxyphenyl) prop-2-en-1-on with the microwave irradiation method and explore some of the biological a

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25

Ghafary, Shahrzad, Hamid Nadri, Mohammad Mahdavi, et al. "Anticholinesterase Activity of Cinnamic Acids Derivatives: In Vitro, In Vivo Biological Evaluation, and Docking Study." Letters in Drug Design & Discovery 17, no. 8 (2020): 965–82. http://dx.doi.org/10.2174/1570180817666191224094049.

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Background: Acetylcholine deficiency in the hippocampus and cortex, aggregation of amyloid-beta, and beta-secretase overactivity have been introduced as the main reasons in the formation of Alzheimer’s disease. Objective: A new series of cinnamic derived acids linked to 1-benzyl-1,2,3-triazole moiety were designed, synthesized, and evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities. Methods: Colorimetric Ellman’s method was used for the determination of IC50% of AchE and BuChE inhibitory activity. The kinetic studies, neuroprotective activit

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26

Çevik, Ulviye Acar, Derya Osmaniye, Serkan Levent, et al. "Synthesis and biological evaluation of novel 1,3,4-thiadiazole derivatives as possible anticancer agents." Acta Pharmaceutica 70, no. 4 (2020): 499–513. http://dx.doi.org/10.2478/acph-2020-0034.

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AbstractThe synthesis of new N-(5-substituted-1,3,4-thiadiazol-2-yl)-2-[(5-(substituted amino)-1,3,4-thiadiazol-2-yl)thio]acetamide derivatives and investigation of their anticancer activities were the aims of this work. All the new compounds’ structures were elucidated by elemental analyses, IR, 1H NMR, 13C NMR and MS spectral data. Anticancer activity studies of the compounds were evaluated against MCF-7 and A549 tumor cell lines. In addition, with the purpose of determining the selectivity of cytotoxic activities, the most active compound was screened against a noncancer NIH3T3 cell line (m

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27

Bouquet, Jérome, Marion Rivaud, Séverine Chevalley, Eric Deharo, Valérie Jullian, and Alexis Valentin. "Biological activities of nitidine, a potential anti-malarial lead compound." Malaria Journal 11, no. 1 (2012): 67. http://dx.doi.org/10.1186/1475-2875-11-67.

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28

Ramadan, M. F., M. M. S. Asker, and Z. K. Ibrahim. "Functional bioactive compounds and biological activities of Spirulina platensis lipids." Czech Journal of Food Sciences 26, No. 3 (2008): 211–22. http://dx.doi.org/10.17221/2567-cjfs.

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The compositions and concentrations of lipid classes, fatty acids, tocopherols were determined in the lipids from blue-green microalga <i>Spirulina platensis</i>. Total lipids (TL) recovered using chloroform: methanol (2:1, v/v) were found to be 163.5 g/kg (on dry weight basis). The level of neutral lipids was the highest, followed by glycolipids and phospholipids, respectively. Among TL and lipid classes, palmitic, &gamma;-linolenic and linoleic acids were the dominating fatty acids. Compared to the neutral lipids, the polar fractions were generally characterised by higher per

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29

Ha, Zhe Y., Hoay C. Ong, Chuan W. Oo, and Keng Y. Yeong. "Synthesis, Molecular Docking, and Biological Evaluation of Benzimidazole Derivatives as Selective Butyrylcholinesterase Inhibitors." Current Alzheimer Research 17, no. 13 (2021): 1177–85. http://dx.doi.org/10.2174/1567205018666210218151228.

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Background: Benzimidazole is an interesting pharmacophore which has been extensively studied in medicinal chemistry due to its high affinity towards various enzymes and receptors. Its derivatives have been previously shown to possess a wide range of biological activities including anthelmintic, antihypertensive, antiulcer, as well as anticholinesterase activity. Objective: The objective of this study is to search for more potent benzimidazole-based cholinesterase inhibitors, through the modification of the 1- and 2-positions of the benzimidazole core. Methods: Synthesis of compounds were carri

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Xin, Fengli, Chunhua Du, Gongjia Lan, and Zhuanping Wu. "Synthesis, Characterization, and Agricultural Biological Activities of 5-Fluoro-2-hydroxy Butyrophenone." Journal of Chemistry 2013 (2013): 1–5. http://dx.doi.org/10.1155/2013/895892.

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A novel synthetic approach towards 5-fluoro-2-hydroxy butyrophenone is reported. Using 4-fluorophenol as a raw material, the processes of etherification protection, Friedel-Crafts acylation and demethylation provide the target compound under mild conditions. The structure was characterized by the melting point and IR, MS,1H-NMR, and13C-NMR spectroscopy. The bioassay results indicate that the target compound exhibits potent antifungal activities againstValsa mali,Coniella dipodiella, and other agricultural plant fungi. The target compound also shows potent herbicidal activities forLactuca sativ

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Jin, Hao, Bai-Xu Wu, Quan Zheng, et al. "Design, synthesis, biological evaluation and docking study of novel quinazoline derivatives as EGFR-TK inhibitors." Future Medicinal Chemistry 13, no. 7 (2021): 601–12. http://dx.doi.org/10.4155/fmc-2020-0015.

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Background: Quinazoline-based compounds have been proved effective in the treatment of cancers for years. Materials & methods: The structural features of several inhibitors of EGFR were integrated and quinazolines with a benzazepine moiety at the 4-position were constructed. Results: Most of the compounds exhibited excellent antitumor activities. Compound 33e showed excellent antitumor activities against the four tested cell lines (IC50: 1.06–3.55 μM). The enzymatic, signaling pathways and apoptosis assay of 33e were subsequently carried out to study the action of the mechanism. Conclusion

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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 (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 </s

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Chan, T. H., Y. J. Zhang, F. Sauriol, A. W. Thomas, and G. M. Strunz. "Studies in iridoid chemistry and spruce budworm (Choristoneurafumiferana) antifeedants." Canadian Journal of Chemistry 65, no. 8 (1987): 1853–58. http://dx.doi.org/10.1139/v87-311.

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34

Pouramiri, Behjat, Mahboobeh Zahedifar, Adileh Ayati, Farah Pouramiri, and Mahdiyeh Ahmadi. "Design, synthesis and biological evaluation of new substituted benzofuran-based derivatives via C−H bond activation." Journal of the Serbian Chemical Society 85, no. 11 (2020): 1405–15. http://dx.doi.org/10.2298/jsc191231039p.

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A series of biologically active disubstituted benzofuran derivatives (3a?d) have been designed and synthesized via C?H bond activation reaction. The chemical structures of all final compounds were confirmed by spectroscopic methods. In vitro anti acetylcholinesterase (AChE) activities of these novel compounds were evaluated and showed low to moderate results. Among them, compound 3d moderately inhibited AChE activities with 68.12 % value.

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Jayanna, N. D., H. M. Vagdevi, J. C. Dharshan, T. R. Prashith Kekuda, B. C. Hanumanthappa, and B. C. Gowdarshivannanavar. "Synthesis and Biological Evaluation of Novel 5,7-Dichloro-1,3-benzoxazole Derivatives." Journal of Chemistry 2013 (2013): 1–9. http://dx.doi.org/10.1155/2013/864385.

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A new class of 5,7-dichloro-1,3-benzoxazole derivatives4–11were synthesized by fusing 5,7-dichloro-2-hydrazino-1,3-benzoxazole3nucleus with aliphatic acids, active methylene compounds, and with selected esters to form heterocyclic ring systems like 1,2,4-triazoles, pyrazoles, and triazine moieties. The compound3on diazotization reaction affords the tetrazole compound. The synthesized compounds were characterized by1H NMR, IR, Mass, and13C NMR spectral data and screened for cytotoxic, antimicrobial, antioxidant, and antilipase activities. The compounds4,5, and8have shown significant antimicrobi

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Abdellattif, Magda H., Mohd Shahbaaz, M. M. H. Arief, and Mostafa A. Hussien. "Oxazinethione Derivatives as a Precursor to Pyrazolone and Pyrimidine Derivatives: Synthesis, Biological Activities, Molecular Modeling, ADME, and Molecular Dynamics Studies." Molecules 26, no. 18 (2021): 5482. http://dx.doi.org/10.3390/molecules26185482.

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In this study, we used oxazinethione as a perfect precursor to synthesize new pyrimidine and pyrazole derivatives with potent biological activities. Biological activities were determined for all compounds against A. flavus, E. coli, S. aureus, and F. moniliform. Compounds 3, 4a-b, and 5 exhibited higher activities toward A. flavus, E. coli, S. aureus, and F. moniliform; this was indicated through the MIC (minimum inhibitory concentration). At the same time, anticancer activities were determined through four cell lines, Ovcar-3, Hela, MCF-7, and LCC-MMk. The results obtained indicated that comp

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Journal, Baghdad Science. "Synthesis and study of biological activity of some new Imidazole derivatives." Baghdad Science Journal 13, no. 3 (2018): 547–55. http://dx.doi.org/10.21123/bsj.13.3.547-555.

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In this work ester derivatives were synthesized by the reaction of imidazole derivatives (C1) with ethylchloroacetate in ethanol and NaOH to give the corresponding (C2) .While compound (C3) acetohydrazide was synthesized by the reaction of ester derivatives (C2) with hydrazine hydrat in ethanol. Compound (C3) from the reaction with different aromatic aldehydes in absolute ethanol gave the Schiff′s bases (C4,C5). The product compounds were characterized by FT-IR, U.V and 1HNMR spectra and the biological activities were studied as antibacterial.

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Yang, Lifang, Xuemei Qin, Hongcun Liu, Yanye Wei, Hailiang Zhu, and Mingguo Jiang. "Design, synthesis and biological evaluation of a series of new resveratrol analogues as potential anti-cancer agents." Royal Society Open Science 6, no. 9 (2019): 190125. http://dx.doi.org/10.1098/rsos.190125.

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A series of novel resveratrol derivatives were designed, synthesized and evaluated as anti-cancer agents. Most of the compounds showed significant anti-proliferative activities against three human cancer cell lines (HepG2, A549 and Hela). Among these compounds, compound r displayed the most potent inhibitory activity and showed low cytotoxic activity. Cell apoptosis and cell cycle assays demonstrated that compound r significantly induced apoptosis ( p < 0.001) and arrested cell cycle at S phase. Immunofluorescence microscopy analysis showed compound r disrupted the tubulin network. Docking

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Yu, Lide, Qinqin Wang, Caolin Wang та ін. "Design, Synthesis, and Biological Evaluation of Novel Thienopyrimidine Derivatives as PI3Kα Inhibitors". Molecules 24, № 19 (2019): 3422. http://dx.doi.org/10.3390/molecules24193422.

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Three series of novel thienopyrimidine derivatives 9a–l, 15a–l, and 18a–h were designed and synthesized, and their IC50 values against four cancer cell lines HepG-2, A549, PC-3, and MCF-7 were evaluated. Most compounds show moderate cytotoxicity against the tested cancer cell lines. The most promising compound 9a showed moderate activity with IC50 values of 12.32 ± 0.96, 11.30 ± 1.19, 14.69 ± 1.32, and 9.80 ± 0.93 µM, respectively. The inhibitory activities of compounds 9a and 15a against PI3Kα and mTOR kinase were further evaluated. Compound 9a exhibited PI3Kα kinase inhibitory activity with

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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 (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

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Zheng, Tao, Yan-Yong Ming, Zheng-Chao Tu, Fu Rong Xu, and Yong-Xian Cheng. "Two New Compounds from Medicinal Insect Blaps japanensis and Their Biological Evaluation." Natural Product Communications 13, no. 2 (2018): 1934578X1801300. http://dx.doi.org/10.1177/1934578x1801300210.

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Blaps japanensis is a medicinal insect used for the treatment of a variety of disorders in Yi-nationality of Yunnan province, China. In the present study, two new compounds, named pipajiains F and G (1 and 2), along with four known compounds, 3-indolealdehyde (3), L-tryptophan (4), ginsenine (5), and anoectochine (6) were isolated from B. japanensis. Their structures were identified on the basis of spectroscopic methods. Compound 1 is a phenolic compound bearing a pyridine-1-ium-1carboxylate motif in the structure which made 1 an unusual architecture. Compounds 2 is an indole alkaloid derivati

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Chhikara, Bhupender S., M. Sudershan Rao, V. Kameshwara Rao, et al. "Carbocyclodipeptides as modified nucleosides: synthesis and anti-HIV activities." Canadian Journal of Chemistry 92, no. 12 (2014): 1145–49. http://dx.doi.org/10.1139/cjc-2014-0356.

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A new class of nucleoside analogues were synthesized using cyclic dipeptides and modified 2′-deoxyfuranoribose sugars to introduce flexibility by peptides in place of common nucleoside bases and to determine their biological properties. The synthesis was carried out by coupling of a protected ribose sugar with synthesized dipeptides in the presence of hexamethyldisilazane and trimethylsilyltriflate. The final products were characterized by NMR and high-resolution MS-TOF spectroscopy. The compounds were evaluated for anti-HIV activities. 1-(4-Azido-5-(hydroxymethyl)tetrahydrofuran-2-yl)-3,6-dii

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Hosseinzadeh, Zahra, Ali Ramazani, Kamaleddin Hosseinzadeh, Nima Razzaghi-Asl, and Farideh Gouranlou. "An Overview on Chemistry and Biological Importance of Pyrrolidinone." Current Organic Synthesis 15, no. 2 (2018): 166–78. http://dx.doi.org/10.2174/1570179414666170908165445.

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Background: Pyrrolidinone is a five membered heterocyclic ring that is a versatile lead compound for designing powerful bioactive agents. Pyrrolidinone nucleus is one of the most important heterocyclic compound indicating notable pharmaceutical effects. Many procedures for the preparation of pyrrolidinone and also their various reactions offer great scope in the field of medicinal chemistry. This fascinating group of compounds has diverse pharmacological activities such as antibacterial, antifungal, anticancer and anticonvulsant. Objective: The review article proposes to classify comprehensive

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Peerzade, Nargisbano A., Shravan Y. Jadhav, and Raghunath B. Bhosale. "Synthesis and Biological Evaluation of Some Novel Quinoline based Chalcones as Potent Antimalarial, Anti-inflammatory, Antioxidant and Antidiabetic Agents." Asian Journal of Chemistry 32, no. 4 (2020): 959–64. http://dx.doi.org/10.14233/ajchem.2020.22542.

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The objective of the present study was to synthesize a series of some novel quinoline based methoxy substituted chalcones and to evaluate their in vitro antimalarial, anti-inflammatory, antioxidant and antidiabetic activitites. The quinoline based chalcones was synthesized by condensation of 2-chloro-3-formyl qunoline with various methoxy substituted acetophenone in presence of NaOH. The Claisen-Schmidt condensation gave high yield of quinoline based chalcones. Synthesis of 2-chloro-3-formyl quinoline was carried out by Vilsmeir-Haack reaction on acetanilide and 4-methoxy acetanilide which on

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Orazbekov, Yerkebulan, Mohamed A. Ibrahim, Serjan Mombekov, et al. "Isolation and Biological Evaluation of Prenylated Flavonoids from Maclura pomifera." Evidence-Based Complementary and Alternative Medicine 2018 (2018): 1–8. http://dx.doi.org/10.1155/2018/1370368.

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Phytochemical analysis of the ethanolic extract of Maclura pomifera fruits yielded four new compounds (I–IV) along with eleven known compounds (V–XV). The crude extract exhibited significant activity towards cannabinoid receptors (CB1: 103.4% displacement; CB2: 68.8% displacement) and possibly allosteric interaction with δ and μ opioid receptors (−49.7 and −53.8% displacement, resp.). Compound I was found to be possibly allosteric for κ and μ opioid receptors (−88.4 and −27.2% displacement, resp.) and showed moderate activity (60.5% displacement) towards CB1 receptor. Compound II exhibited mod

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Zhang, Hua-Sheng, Yong-Ming Yan, Dai-Wei Wang, Qing Lv, Yong-Xian Cheng, and Shu-Mei Wang. "Small Molecule Constituents of Periplaneta americana and Their IL-6 Inhibitory Activities." Natural Product Communications 16, no. 9 (2021): 1934578X2110331. http://dx.doi.org/10.1177/1934578x211033180.

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Two new glycosides, periplanosides A (1) and B (2), 3 compounds reported from a natural source for the first time (3 − 5), and 6 known compounds 6 − 11 were isolated from the ethanol extract of Periplaneta americana (Linnaeus). Their structures, including absolute configurations, were unambiguously identified by comprehensive spectroscopic and chemical methods. Compound 3 is a racemate whose enantiomers were purified by chiral high-performance liquid chromatography . The biological evaluation results showed that compound 7 (0 − 20 μM) did not affect the viability of RAW264.7 cells and could ef

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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 (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 comp

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Wang, Xiaohong, Rui Jiang, Zizhen Liu, et al. "Phytochemicals and Biological Activities of Poisonous Genera of Ericaceae in China." Natural Product Communications 9, no. 3 (2014): 1934578X1400900. http://dx.doi.org/10.1177/1934578x1400900333.

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The family Ericaceae is comprised of about 70 genera of which about 20 are found throughout China. Of these Ledum, Rhododendron, Enkianthus, Pieris, Craibiodendron, Gaultheria, Vaccinium, and Leucothoe are regarded as poisonous. Many species of these poisonous genera are used as Chinese herbal medicines for the treatment of, for example, inflammation, asthma, and coughs. Modern research has demonstrated that the toxic ingredients of these poisonous genera are chiefly tetracyclic diterpenes, which have adverse effects on the digestive, cardiovascular and nervous systems. Because various species

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Glamočlija, Una, Subhash Padhye, Selma Špirtović-Halilović, et al. "Synthesis, Biological Evaluation and Docking Studies of Benzoxazoles Derived from Thymoquinone." Molecules 23, no. 12 (2018): 3297. http://dx.doi.org/10.3390/molecules23123297.

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Thymoquinone (TQ), a natural compound with antimicrobial and antitumor activity, was used as the starting molecule for the preparation of 3-aminothymoquinone (ATQ) from which ten novel benzoxazole derivatives were prepared and characterized by elemental analysis, IR spectroscopy, mass spectrometry and NMR (1H, 13C) spectroscopy in solution. The crystal structure of 4-methyl-2-phenyl-7-isopropyl-1,3-benzoxazole-5-ol (1a) has been determined by X-ray diffraction. All compounds were tested for their antibacterial, antifungal and antitumor activities. TQ and ATQ showed better antibacterial activit

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Niu, Tianyu, Xiaoqiang Zhao, Jing Jiang, et al. "Evolution and Biological Evaluation of Matrinic Derivatives with Amantadine Fragments As New Anti-Influenza Virus Agents." Molecules 24, no. 5 (2019): 921. http://dx.doi.org/10.3390/molecules24050921.

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A series of novel tricyclic matrinic derivatives with 11-adamantyl substitution were designed, synthesized, and evaluated for their activities against Influenza A H3N2 virus, based on the privileged structure strategy. Structure-activity relationship (SAR) analysis indicated that the introduction of an 11-adamantyl might be helpful for the potency. Among them, compounds 9f and 9j exhibited the promising anti-H3N2 activities with IC50 values of 7.2 μM and 10.2 μM, respectively, better than that of lead 1. Their activities were further confirmed at the protein level. Moreover, compound 9f displa

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