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کاربرد نوع شرط:
- جایگاه : پژوهشی
- مجله: Asian Journal of Green Chemistry
- نوع مقاله: Journal Article
- کلمات کلیدی: 3,Benzotriazole 1,4-oxadiazole Hydrazone Antitubercular Anticancer
- چکیده:
- چکیده انگلیسی: The development of novel compounds, hydrazones have shown that they possess a wide variety of biological activities. Hydrazones/azomethines/imines possess -NHN=CH- and constitute an important class of compounds for new drug development. We have undertaken a library synthesis of (1H-benzo[d][1,2,3]triazole-5-yl)(phenyl) methanone clubbed 1,3,4-oxadiazole derivatives bearing substituted hydrazone moiety were synthesized. We have synthesized a collection of 14 compounds and characterized by elemental analysis, MS, 1H NMR, and 13C NMR spectral data and were screened, against the anticancer and antituberculosis activity. Where the majority of these compounds showed good anticancer and antitubercular activities against the tested strains of M. tuberculosis H37Rv and lung NCI H-522, ovary PA-1, liver Hep G2 compared with the reference drugs. Compounds 5d, 5e, 5g, and 5n showed excellent potency against M. tuberculosis H37Rv strain compares to standard drugs whereas, against lung NCI H-522 cancer cell lines compounds 5e, against ovary PA-1 cancer cell line compound 5i, and against liver Hep G2 cell line compound 5n showed excellent activity compared to standard drug thus, these studies suggest that (1H-benzo[d][1,2,3]triazol-5-yl)(phenyl)methanone clubbed 1,3,4-oxadiazole derivatives bearing hydrazone moiety are interesting scaffolds for the development of novel antitubercular and anticancer agents.
- انتشار مقاله: 14-05-1398
- نویسندگان: Keyur M. Pandya,Bhavesh P. Dave,Arpan H. Patel,Rajesh J. Patel,Jignesh T. Patel,Piyush S. Desai
- مشاهده
- جایگاه : پژوهشی
- مجله: Advanced Journal of Chemistry-Section A
- نوع مقاله: Journal Article
- کلمات کلیدی: Antibacterial,1,Antifungal,Antituberculosis,Benzotriazole,3,4-Oxadiazoles
- چکیده:
- چکیده انگلیسی: In this research study, we have synthesized a library of 2-substituted-1-(2-(5-((5-5-benzoyl-1H-benzo[d][1,2,3]triazole-1-yl)methyl)-2-thioxo-1,3,4-oxadiazol-3(2H)-yl) acetamido)-5-oxo-2,5-dihydro-1H-pyrrole-3-carboxylic acids from 1H-benzo[d][1,2,3] triazole-5-yl)(phenyl)methanone. The synthesized compounds were characterized using 1H NMR, 13C NMR, C,H,N elemental analysis and mass spectroscopy studies. All the compounds were investigated for their in silico ADME prediction properties, in vitro antibacterial activity against four bacterial strains, antifungal activity against two fungal strains, and antimycobacterial activity against the H37Rv. All the compounds revealed good to moderate activity against the bacterial strain. Among all the compounds, 6b and 6f showed better antimycobacterial agents compared with that of the standard drug ciprofloxacin and pyrazinamide, whereas 6a, 6b, and 6e were found to be excellent antifungal and antibacterial agent compared standard drugs clotrimazole and ciprofloxacin. The results of the in-silico analysis depicted that the synthesized compounds had excellent drug-likeness properties.
- انتشار مقاله: 01-07-1398
- نویسندگان: Keyur Pandya,Bhavesh Dave,Rajesh Patel,Piyush Desai
- مشاهده