Synthetic approaches, structure activity relationship and biological applications for pharmacologically attractive pyrazole/pyrazoline-thiazolidine-based hybrids

Eur J Med Chem. 2016 May 4:113:145-66. doi: 10.1016/j.ejmech.2016.02.030. Epub 2016 Feb 16.

Abstract

The features of the chemistry of 4-thiazolidinone and pyrazole/pyrazolines as pharmacologically attractive scaffolds were described in a number of reviews in which the main approaches to the synthesis of mentioned heterocycles and their biological activity were analyzed. However, the pyrazole/pyrazoline-thiazolidine-based hybrids as biologically active compounds is poorly discussed in the context of pharmacophore hybrid approach. Therefore, the purpose of this review is to summarize the data about the synthesis and modification of heterocyclic systems with thiazolidine and pyrazoline or pyrazole fragments in molecules as promising objects of modern bioorganic and medicinal chemistry. The description of biological activity was focused on SAR analysis and mechanistic insights of mentioned hybrids.

Keywords: Biological activity; Pyrazole; Pyrazoline; Synthesis; Thiazolidine.

Publication types

  • Review

MeSH terms

  • Chemistry, Pharmaceutical
  • Molecular Structure
  • Pyrazoles / chemistry
  • Pyrazoles / pharmacology*
  • Structure-Activity Relationship
  • Thiazolidines / chemistry
  • Thiazolidines / pharmacology*

Substances

  • Pyrazoles
  • Thiazolidines
  • pyrazole