Inhibitory activities of indolizine derivatives: a patent review

Expert Opin Ther Pat. 2020 Sep;30(9):695-714. doi: 10.1080/13543776.2020.1798402. Epub 2020 Aug 1.

Abstract

Introduction: Indolizines are structural isomers with indoles. Although several indole-based commercial drugs are available in the market, none of the indolizine-based drugs are available up-to-date. Natural and synthetic indolizines have a wide-range of pharmaceutical importance such as antitumor, antimycobacterial, antagonist, and antiproliferative activities. This prompted us to search and collect all possible data about the pharmacological importance of indolizine to open an avenue to the researchers in exploring more medicinal applications of such biologically important compounds.

Areas covered: The current review article covers the advancements in the biological and pharmacological activities of indolizine-based compounds during the last decade. The covered areas of this work involved anticancer, anti-HIV-1, anti-inflammatory, antimicrobial, anti-tubercular, larvicidal, anti-schizophrenia, CRTh2 antagonist's activities in addition to enzymatic inhibitory activity.

Expert opinion: The discovery of indolizine drugs will be a major breakthrough as compared with their widely available drug-containing indole isosteres. Major work collected here was focused on anticancer, anti-tubercular, anti-inflammatory, and enzymatic inhibitory activities. The SAR study of the reported biologically active indolizines is summarized throughout the review whenever highlighted to the rationale the behavior of inhibitory action. Several indolizines with certain functions provided great enhancement in the therapeutic activities comparing with reference drugs.

Keywords: Indolizines; anti-HIV; anticancer; antiinflammatory; antitubercular; enzymes inhibitors.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Design*
  • Drug Discovery
  • Humans
  • Indolizines / chemistry
  • Indolizines / pharmacology*
  • Patents as Topic
  • Structure-Activity Relationship

Substances

  • Indolizines