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Design, synthesis, and evaluation of new α‐aminonitrile‐based benzimidazole biomolecules as potent antimicrobial and antitubercular agents
Author(s) -
Shaikh Irfan N.,
Hosamani Kallappa M.,
Kurjogi Mahantesh M.
Publication year - 2018
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201700205
Subject(s) - antimicrobial , benzimidazole , chemistry , benzaldehyde , antifungal , combinatorial chemistry , catalysis , salicylaldehyde , cytotoxicity , sodium cyanide , organic chemistry , cyanide , stereochemistry , microbiology and biotechnology , biochemistry , in vitro , biology , schiff base
Abstract The study explores the one‐pot synthesis of novel α‐aminonitriles by reacting 4‐[(1 H ‐benzimidazol‐2‐yl)methoxy]benzaldehyde, substituted anilines and sodium cyanide using a catalytic amount of copper dipyridine dichloride (CuPy 2 Cl 2 ) and employing the Strecker reaction under mild conditions. All the synthesized compounds were screened for antimicrobial and antitubercular activity. The promising lead compounds 4d and 4e were identified, with MIC values ranging between 3.9 and 7.8 µg/mL against different bacterial strains. Compounds 4c–e and 4g also showed good antifungal activities against the tested fungal strain. Among those tested, compound 4e exhibited excellent antitubercular activity (MIC 0.05 μg/mL) with a low level of cytotoxicity, suggesting that compound 4e is a promising lead for subsequent investigations in search for new antitubercular agents.