期刊
CHEMICAL BIOLOGY & DRUG DESIGN
卷 81, 期 2, 页码 219-227出版社
WILEY
DOI: 10.1111/cbdd.12065
关键词
anti-TB activity; cytotoxicity; dihydropyrimidine; single crystal X-ray crystallography
资金
- NRF South Africa for DST/NRF Innovation Postdoctoral Fellowship
A series of 2-(substituted phenyl/benzyl-amino)-6-(4-chlorophenyl)-5-(methoxycarbonyl)-4-methyl-3,6-dihydropyrimidin-1-ium chlorides 713 and 15 was synthesized in their hydrochloride salt form. The title compounds were characterized by FT-IR, NMR (1H and 13C) and elemental analysis. They were evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv, multidrug resistance tuberculosis and extensively drug resistance tuberculosis by agar diffusion method and tested for the cytotoxic action on peripheral blood mononuclear cells by MTT assay. Among all the tested compounds in the series, compounds 7 and 11 emerged as promising antitubercular agents at 16 mu g/mL against multidrug resistance tuberculosis and over 64 mu g/mL against extensively drug resistance tuberculosis. The conformational features and supramolecular assembly of the promising compounds 7 and 11 were determined by single crystal X-ray study.
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