Synthesis and Antituberculosis Activity of New Hydrazide Derivatives

KAPLANCIKLI Z. A., Turan-Zitouni G., ÖZDEMİR A., Teulade J.

ARCHIV DER PHARMAZIE, cilt.341, sa.11, ss.721-724, 2008 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 341 Sayı: 11
  • Basım Tarihi: 2008
  • Doi Numarası: 10.1002/ardp.200800048
  • Dergi Adı: ARCHIV DER PHARMAZIE
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Index Chemicus (IC)
  • Sayfa Sayıları: ss.721-724
  • Anahtar Kelimeler: Antituberculosis activity, Hydrazide, Imidazo[1,2-a]pyridine, ANTIMYCOBACTERIAL ACTIVITY, IN-VITRO, TUBERCULOSIS, TB
  • Anadolu Üniversitesi Adresli: Evet

Özet

The increasing clinical importance of drug-resistant mycobacterial pathogens, especially Mycobacterium tuberculosis, has lent additional urgency to microbiological research and new antimycobacterial compound development. For this purpose, new hydrazide derivatives of imidazo[1,2-a]pyridine were synthesized and evaluated for antituberculosis activity. The reaction of 2-[(2-carboxyimidazo[1,2-a]pyridine-3-yl)sulfanyl]acetic acid hydrazide with various benzaldehydes gave N-(arylidene)-2-[(2-carboxyimidazo[1,2-a]pyridine-3-yl)sulfanyl]acetic acid hydrazide derivatives. The chemical structures of the compounds were elucidated by IR, H-1-NMR, FAB-MS spectral data and elemental analysis. Anti tuberculosis activities of the synthesized compounds were determined by broth microdilution assay, the Microplate Alamar Blue Assay in BACTEC 12B medium. The results were screened in vitro, using the BACTEC 460 Radiometric System against Mycobacterium tuberculosis H37Rv (ATCC 27294) at 6.25 mu g/mL; the tested compounds showed significant inhibition.