Synthesis and evaluation of new imidazo[2,1-b]thiazoles as antituberculosis agents


Ulusoy Guzeldemirci N., Gursoy E.

MARMARA PHARMACEUTICAL JOURNAL, cilt.21, sa.1, ss.102-109, 2017 (ESCI) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 21 Sayı: 1
  • Basım Tarihi: 2017
  • Doi Numarası: 10.12991/marupj.259887
  • Dergi Adı: MARMARA PHARMACEUTICAL JOURNAL
  • Derginin Tarandığı İndeksler: Emerging Sources Citation Index (ESCI), Scopus, TR DİZİN (ULAKBİM)
  • Sayfa Sayıları: ss.102-109
  • Anahtar Kelimeler: Imidazo[2,1-b]thiazole, hydrazone, antimycobacterial activity, ANTIMYCOBACTERIAL ACTIVITY, DERIVATIVES, SYSTEM
  • İstanbul Üniversitesi Adresli: Evet

Özet

New N'-(arylidene)-2-[6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl]acetohydrazides (3a-i) were synthesized by reacting 2-[6-(4-bromophenyl) imidazo[2,1-b] thiazol-3-yl] acetohydrazide with different aromatic aldehydes. The structures of the title compounds were established by spectral data (IR, H-1 NMR, C-13 NMR) and elemental analyses. The synthesized compounds were evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv employing the BACTEC 460 radiometric system. The compounds exhibited varying degrees of inhibition in the in vitro primary screening that was conducted at a concentration of 6.25 mu g/ml. Among the synthesized compounds [6-(4-bromophenyl) imidazo[2,1-b]thiazol-3-yl]acetic acid 2,4-dinitrobenzylidenehydrazide (3e) was found to be the most active compound in vitro with MIC of 6.25 mu g/ml.