期刊
SYNTHETIC COMMUNICATIONS
卷 49, 期 16, 页码 2017-2028出版社
TAYLOR & FRANCIS INC
DOI: 10.1080/00397911.2019.1614630
关键词
Antitubercular activity; click chemistry; molecular docking study; N-phenylacetamide; phthalimide; 1,2,3-triazole
资金
- UGC Junior Research Fellowship (JRF) [2061410333, 22/06/2014 (i) EU-V]
In a search for safer and potent antitubercular agents, here a library of newly substituted dioxoisoindolinylmethyl-triazolyl-N-phenylacetamide derivatives (5a-l) has been synthesized via click chemistry approach. All synthesized compounds were evaluated for their antitubercular activity against Mycobacterium tuberculosis H(37)Rv (MTB). Among the screened compounds, 5d, 5e, 5h, and 5l showed good antitubercular activity. The compounds 5d and 5l have shown very effective antitubercular activity against Mycobacterium tuberculosis H(37)Rv (MTB) with MIC 12.5 mu g/mL. All the newly synthesized compounds were thoroughly characterized by H-1 NMR, C-13 NMR, and HRMS spectral data. We further performed exploratory docking studies on the crystal structure of Mycobacterium tuberculosis enoyl reductase to demonstrate the mechanism of antitubercular activity.
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