Thiazolidin-4-one-based derivatives - Efficient tools for designing antiprotozoal agents. A review of the last decade

Bioorg Chem. 2023 Apr:133:106398. doi: 10.1016/j.bioorg.2023.106398. Epub 2023 Jan 30.

Abstract

Thiazolidin-4-one derivatives have a wide range of therapeutic implementations and clinical significance for medicinal chemistry. This heterocyclic ring has been reported to possess a variety of biological activities, including antiprotozoal activities that have inspired scientists to integrate this scaffold with different pharmacophoric fragments to design novel and effective antiprotozoal compounds. There are reviews describing thiazolidin-4-ones small molecules as good candidates with a single type of antiprotozoal activity, but none of these show collected news associated with the antiprotozoal activity of thiazolidin-4-ones and their SAR analysis from the last decade. In this review we are focusing on the antitoxoplasmic, anti-trypanosomal, antimalarial, antileishmanial, and antiamoebic activity of these derivatives, we attempt to summarize and analyze the recent developments with regard to the antiprotozoal potential of 4-TZD covering the structure-activity relationship and main molecular targets. The importance of various structural modifications at C2, N3, and C5 of the thiazolidine-4-one core has also been discussed in this review. We hope that all information concluded in this review can be useful for other researchers in constructing new effective antiprotozoal agents.

Keywords: Anti-Toxoplasma gondii activity; Anti-trypanosomal activity; Antiamoebic activity; Antileishmanial activity; Antimalarial activity; Antiprotozoal agents; Thiazolidin-4-ones.

Publication types

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

MeSH terms

  • Antimalarials* / pharmacology
  • Antimalarials* / therapeutic use
  • Antiprotozoal Agents* / chemistry
  • Structure-Activity Relationship
  • Thiazolidines / chemistry

Substances

  • Antiprotozoal Agents
  • Thiazolidines
  • Antimalarials