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Design, Synthesis, and Biological Evaluation of 1,4‐dihydropyridine Derivatives as Potent Antitubercular Agents
Author(s) -
Desai Nisheeth C.,
Trivedi Amit R.,
Somani Hardik C.,
Bhatt Kandarp A.
Publication year - 2015
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12502
Subject(s) - imidazole , cytotoxicity , chemistry , isoniazid , dihydropyridine , mycobacterium tuberculosis , stereochemistry , moiety , nuclear magnetic resonance spectroscopy , combinatorial chemistry , biological activity , organic chemistry , biochemistry , tuberculosis , calcium , in vitro , medicine , pathology
A series of novel 1,4‐dihydropyridine‐3,5‐dicarbamoyl derivatives bearing an imidazole nucleus at C‐4 position were synthesized in excellent yields via multicomponent Hantzsch reaction. The newly synthesized compounds were characterized by IR , 1 H NMR , 13 C NMR , and mass spectroscopy. The synthesized compounds 3a‐p were screened for antitubercular activity. Among all the screened compounds, compounds 3j and 3m showed most prominent activity against Mycobacterium tuberculosis with minimum inhibitory concentration of 0.02 μ g/mL and SI > 500, making it more potent than first‐line antitubercular drug isoniazid. In addition, these compounds displayed relatively low cytotoxicity.