Recent advances in the development of cinnamic-like derivatives as antituberculosis agents

Expert Opin Ther Pat. 2012 Feb;22(2):155-68. doi: 10.1517/13543776.2012.661717. Epub 2012 Feb 14.

Abstract

Introduction: The high susceptibility of human immunodeficiency virus-infected people to tuberculosis (TB), the emergence of multi-drug-resistant (MDR-TB) strains and extensively drug-resistant (XDR-TB) ones, has brought TB into the focus of urgent scientific interest. As a result, there has been an upsurge in recent years to find new anti-TB agents, with the cinnamoyl moiety having been identified as a particularly simple and effective pharmacophore for this purpose.

Areas covered: This review aims at highlighting the potential of (non)natural cinnamic derivatives to treat TB. It provides an overview of the worldwide recent patent and literature surrounding this type of easy-to-prepare small molecules. There is a special focus on their salient structural and chemical features involved in the reported anti-TB activities.

Expert opinion: Cinnamic derivatives clearly appear as attractive drug candidates to combat TB. So far, literature has reported that they are easy to synthesize and have promising anti-TB activities. Nevertheless, the mode(s) of action of these small molecules remain(s) to date obscure, which is why the implicated molecular mechanisms deserve to be investigated in further detail in the near future.

Publication types

  • Review

MeSH terms

  • Animals
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacology*
  • Cinnamates / chemistry
  • Cinnamates / pharmacology*
  • Drug Design
  • Humans
  • Legislation, Drug
  • Molecular Structure
  • Patents as Topic
  • Structure-Activity Relationship

Substances

  • Antitubercular Agents
  • Cinnamates