Synthesis and antituberculosis activity of new hydrazide derivatives.
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,(1)H-NMR, FAB-MS spectral data and elemental analysis. Antituberculosis 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 microg/mL; the tested compounds showed significant inhibition.
Kaplancikli
Zafer A
ZA
Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Eskisehir, Turkey.
Turan-Zitouni
Gulhan
G
Ozdemir
Ahmet
A
Teulade
Jean-Claude
JC
D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001547:Benzaldehydes; D002264:Carboxylic Acids; D006834:Hydrazines / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D011725:Pyridines; D013057:Spectrum Analysis; D013329:Structure-Activity Relationship
D000995:Antitubercular Agents; D001547:Benzaldehydes; D002264:Carboxylic Acids; D006834:Hydrazines; D011725:Pyridines