Antimycobacterial evaluation of novel hybrid arylidene thiazolidine-2,4-diones

Ponnuchamy S 1 , Kanchithalaivan S 2 , Ranjith Kumar R 3 , Ali MA 4 , Choon TS 5

Affiliations 

  • 1 Orchid Chemicals & Pharmaceuticals Ltd, R&D Center, Chennai 600119, India
  • 2 Department of Organic Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai 625021, Tamil Nadu, India
  • 3 Department of Organic Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai 625021, Tamil Nadu, India. Electronic address: raju.ranjithkumar@gmail.com
  • 4 Institute for Research in Molecular Medicine, Universiti Sains Malaysia, Minden 11800, Penang, Malaysia; New Drug Discovery Research, Department of Medicinal Chemistry, Alwar Pharmacy College, Alwar, Rajasthan 301030, India; New Drug Discovery Research, Department of Medicinal Chemistry, Sunrise University, Alwar, Rajasthan 301030, India
  • 5 Institute for Research in Molecular Medicine, Universiti Sains Malaysia, Minden 11800, Penang, Malaysia
Bioorg Med Chem Lett, 2014 Feb 15;24(4):1089-93.
PMID: 24472146 DOI: 10.1016/j.bmcl.2014.01.007

Abstract

A series of novel hybrid heterocycles comprising arylidene thiazolidine-2,4-dione and 1-cyclopropyl-2-(2-fluorophenyl)ethanone were synthesized. These compounds were evaluated for their antimycobacterial activity against Mycobacterium tuberculosis H37Rv in High Throughput Screen. Most of the hybrid arylidene thiazolidine-2,4-diones displayed moderate to good activity with MIC of less than 50 μM. Compound 1m exhibited maximum potency being 5.87 fold more active at EC50 and 6.26 fold more active at EC90 than the standard drug pyrimethamine.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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