Structure activity relationship (SAR) study of benzimidazole scaffold for different biological activities: A mini-review

Eur J Med Chem. 2015 Jun 5:97:419-43. doi: 10.1016/j.ejmech.2014.11.053. Epub 2014 Nov 26.

Abstract

Benzimidazoles are the fused heterocyclic ring systems which form an integral part of vitamin B12 and have been luring many researchers all over the world to assess their potential therapeutic significance. They are known for their crucial role in numerous diseases via various mechanisms. Substitution of benzimidazole nucleus is a crucial step in the drug discovery process. Therefore, it is necessary to gather the latest information along with the earlier information to understand the present status of benzimidazole nucleus in drug discovery. In the present review, benzimidazole derivatives with different pharmacological activities are described on the basis of SAR study using structural substitution pattern around the benzimidazole nucleus and aims to review the reported work related to the chemistry and pharmacological activities of benzimidazole derivatives during recent years. The present manuscript to the best of our knowledge is the first compilation on synthesis and medicinal aspects including structure-activity relationships of benzimidazole reported to date.

Keywords: Anthelmintics; Benzimidazole; Heterocyclic ring systems; Pharmacological activities; SAR study.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Benzimidazoles / chemistry*
  • Benzimidazoles / pharmacology*
  • Drug Discovery*
  • Humans
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Benzimidazoles
  • benzimidazole