Imidazole: An Essential Edifice for the Identification of New Lead Compounds and Drug Development

Mini Rev Med Chem. 2018;18(2):142-163. doi: 10.2174/1389557517666170228113656.

Abstract

In recent years, a drastic rise has been observed in incidences of resistance, low efficacy rates and toxicities to various drugs used in therapeutic application. Presence of imidazole nucleus in several categories of therapeutic agents such as anti-microbials, anti-virals, anti-cancer, etc has made it a vital anchor for the development of new therapeutic agents. Still, there is a need to couple the newest information with the already available knowledge to recognize the present standing of imidazole motif in medicinal chemistry research. In the present review, importance of this nucleus in some less explored activities like anti-malarial and anthelmintic is mentioned along with well explored fields like cancer. Substitution pattern around imidazole nucleus is discussed here with an aim to help medicinal chemists for the development of SAR of imidazole based compounds for each activity. This discussion will further help in the advancement of existing imidazole derivatives and in the generation of new and safe imidazole compounds.

Keywords: Anti-cancer; antimicrobial; biological activities; drug development; heterocycles; imidazole.

Publication types

  • Review

MeSH terms

  • Anthelmintics / chemical synthesis
  • Anthelmintics / chemistry
  • Anthelmintics / pharmacology*
  • Antimalarials / chemical synthesis
  • Antimalarials / chemistry
  • Antimalarials / pharmacology*
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Drug Design*
  • Helminthiasis / drug therapy*
  • Humans
  • Imidazoles / chemical synthesis
  • Imidazoles / chemistry
  • Imidazoles / pharmacology*
  • Malaria / drug therapy*
  • Neoplasms / drug therapy*

Substances

  • Anthelmintics
  • Antimalarials
  • Antineoplastic Agents
  • Imidazoles
  • imidazole