title: Synthesis, characterization and evaluation of antituberculosis activity of some hydrazones.
abstract: Several new hydrazone derivatives were prepared by the reaction of some active hydrogen compounds with the diazonium salts of 4-amino-3,5-di/1,3,5-trimethylpyrazoles at 0-5 degrees C. Structures of the new substances were confirmed using UV, IR, 1H NMR, 13C NMR and EI-mass spectral data. In vitro antituberculosis activity of these compounds were tested on Mycobacterium tuberculosis H37Rv at 6.25 microg/ml. Both hydrazone products, ethyl 2-[(3,5-dimethylpyrazole-4-yl)hydrazono]-3-oxobutyrate (3d) and methyl 2-[(3,5-dimethylpyrazole-4-yl)hydrazono]4-methoxy-3-oxobutyrate (3e) showed 29 and 28% inhibition against M. tuberculosis, respectively.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Marmara University, Haydarpaşa, Istanbul, Turkey.
authors.forename: Kaymakçioğlu B
authors.initials: KB
authors.lastname: Koçyiğit
authors.forename: S
authors.initials: S
authors.lastname: Rollas
mesh_terms: D000090:Acetoacetates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004352:Drug Resistance, Microbial; D006835:Hydrazones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*
chemical_list: D000090:Acetoacetates; D000995:Antitubercular Agents; D006835:Hydrazones; C471771:ethyl 2-((3,5-dimethylpyrazole-4-yl)hydrazono)-3-oxobutyrate; C471772:methyl 2-((3,5-dimethylpyrazole-4-yl)hydrazono)4-methoxy-3-oxobutyrate