Benzimidazole‐Based Anthelmintic Drugs: Synthetic Strategy, Pharmacological Insights, and SAR Analysis

Abstract Helminth diseases from parasitic worms create major problems worldwide in human health and farming operations. Benzimidazole derivatives bind specifically to β‐tubulin and serve as essential components in worm treatment medications. Drug researchers need new approaches because current treatments are becoming less effective. This review delves into the pharmacological properties, mechanisms of action, and structure–activity relationships (SAR) of benzimidazole derivatives, with a focus on synthetic modifications such as lipophilic substitutions to enhance membrane permeability and carbamate moiety optimization for improved binding affinity. The review presents the latest drug resistance strategies, which include new delivery systems through nanotechnology and resistance‐overcoming agent combinations. Scientists found that the absorption and safety patterns of albendazole, mebendazole, and triclabendazole work well for parasite control across different treatment locations. The study investigates using modern screening methods and artificial intelligence to discover new treatments against worm infections. Our review discusses new developments to improve benzimidazole antiparasitic medicine for handling increasing parasite infection rates.