Synthesis and biological evaluation of new 4-thiazolidinone derivatives


Guzel O. , Salman A.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol.24, no.4, pp.1015-1023, 2009 (Peer-Reviewed Journal) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 24 Issue: 4
  • Publication Date: 2009
  • Doi Number: 10.1080/14756360802608021
  • Journal Name: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded, Scopus
  • Page Numbers: pp.1015-1023
  • Keywords: thiazolidinone, antimycobacterial activity, antitumor activity, NATIONAL-CANCER-INSTITUTE, MYCOBACTERIUM-TUBERCULOSIS, ANTICONVULSANT ACTIVITY, DRUG DISCOVERY, THIAZOLIDINONE, AGENTS, ASSAY

Abstract

A series of new 2-aryl-4-thiazolidinones (3 and 4) was synthesized from 2-hydroxy-2,2-diphenyl-N'-[(substituted phenyl)methylene]acetohydrazides (2) and mercaptoacetic acid or 2-mercaptopropionic acid. The antimycobacterial activity of these compounds was determined and several leads with 95-99% inhibition at 6.25 mu g/mL test concentration were identified. In addition, antitumor activities were measured against several tumor cell lines, and significant growth inhibition was observed for compound 4p. Taken together, 2-aryl-4-thiazolidinones were shown to be promising scaffolds for both antimycobacterial and tumor-targeting compounds.