An Efficient Synthesis of Novel 2‐(5‐indolyl)‐1H‐benzimidazole Derivatives and Evaluation of Their Antimicrobial Activities

Abstract

In this paper, we report the synthesis of novel 2‐(5‐indolyl)‐1H‐benzimidazole derivatives. The methodology involves the Sonogashira reaction of 4‐(1H‐benzimidazol‐2‐yl)‐2‐bromo‐N,N‐dimethylaniline (3) with variety of terminal alkynes to get corresponding novel 4‐(1H‐benzimidazol‐2‐yl)‐2‐alkynyl‐N,N‐dimethylaniline derivatives (4). These compounds on iodocyclization afforded novel iodoindolylbenzimidazole derivatives (5). The resulting compounds were functionalized further via palladium‐mediated carbon–carbon bond formation for generating novel structurally diversified heterocyclic compounds. All these newly synthesized compounds were evaluated for antimicrobial activity.

New Benzimidazole-1,2,4-Triazole Hybrid Compounds: Synthesis, Anticandidal Activity and Cytotoxicity Evaluation

“…Furthermore, the benzimidazole scaffold has an ability to form hydrogen bonds with biological enzymes and receptors and participates in π–π and hydrophobic interactions, which may be related to its mechanism of action [ 18 , 19 ]. Because of these features, several pharmacological and biochemical research have been performed, and many of them have supported the finding that benzimidazole derivatives are potent against various microorganism strains [ 20 , 21 , 22 , 23 , 24 , 25 , 26 , 27 , 28 , 29 , 30 , 31 , 32 , 33 ]. Benzimidazoles can be classified as one the most important group of fungicides with systemic activity and are well-known for their pronounced ability to control a large number of fungal diseases.…”