An Outline on benzimidazole Containing Marketed Drugs with Proton Pump Inhibitor and H1 Receptor Antagonist Activities

Mini Rev Med Chem. 2025 Jan 6. doi: 10.2174/0113895575329633240928163509. Online ahead of print.

Abstract

Heterocyclic compounds are increasingly used in medicinal chemistry because they are the main components of many biological processes and materials. Benzimidazole remains the core center of the heterocyclic chemical group, with essential traits such as six-five-member connected rings and two nitrogen atoms at the 1,3 position in a six-membered benzene and five-membered imidazole- fused ring system. Molecules with benzimidazole derivatives serve important functions as therapeutic agents and have shown excellent results in clinical and biological research. In this comprehensive review, we summarize marketed medications that include the benzimidazole moiety. Here, we discuss two topics: PPIs and H1 receptor antagonists. Benzimidazole derivatives are important in all fields because they have the same isostructural pharmacophore as that of naturally occurring active biomolecules. While PPIs and H1 receptor antagonists are generally safe in the short term, accumulating data suggest that their long-term use may pose concerns. This systematic review aimed to assess global PPI use in the general population. This will help researchers, medicinal chemists, and pharmaceutical scientists to create breakthrough benzimidazole-based drugs. This review can help identify novel lead compounds and optimize existing benzimidazole derivatives to improve medicinal efficacy. Benzimidazole has attracted significant interest because of its high bioavailability, stability, and biological efficiency. This page reveals and discusses typical synthesis processes for marketed pharmaceuticals in the benzimidazole class of scaffolds, MOA, and therapeutic uses.

Keywords: Adverse effect.; Benzimidazole moiety; H1 receptor antagonist; MOA; PPIs; SAR; marketed drugs; synthetic route; therapeutical uses.