Design, synthesis, and evaluation of new α-aminonitrile-based benzimidazole biomolecules as potent antimicrobial and antitubercular agents.

The study explores the one-pot synthesis of novel α-aminonitriles by reacting 4-[(1H-benzimidazol-2-yl)methoxy]benzaldehyde, substituted anilines and sodium cyanide using a catalytic amount of copper dipyridine dichloride (CuPy2 Cl2 ) 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.

Synthesis and in-vivo evaluation of carbonyl-amide linkage based new benzimidazole derivatives.

In search of pharmacologically active potent compounds, a series of carbonyl-amide linkage based new benzimidazole derivatives were synthesized from acid, aldehydes and isocyanide at ambient temperature via Passerini reaction. All the compounds synthesized were screened for their potential anti-inflammatory, antidiabetic and anticonvulsant properties. The results revealed that compounds 2i and 2j were found to be the most potent anti-inflammatory agents, while compounds 2a, 2c, 2e, 2f, 2i and 2j showed increased antidiabetic activity than the reference drugs and 2a, 2g, 2h, 2i and 2j were found to be the main structural requirement for maintaining anticonvulsant activity.