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A study on synthesis and antimicrobial activity of 4-acyl-pyrazoles
Authors:Adnan Çetin  ?shak Bildirici
Institution:1. Mu? Alparslan University, Faculty of Education, Department of Sciences, Mu?, Turkey;2. Yüzüncü Y?l University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Van, Turkey
Abstract:4-Acyl-pyrazole-3-carboxylic acids (1) were synthesized via the reaction of 4-acyl-2,3-furandiones (F) with hydrazone (1-benzylidene-2-(2,5-dimethyl-phenyl)-hydrazine) by heating under solid phase and their acid chlorides (2) were obtained. Then these derivatives were easily converted into the corresponding derivatives such as ester, amide, ureide, pyrazolo-pyridazine, etc. Totally 62 new compounds were synthesized. The structures of these new synthesized compounds were determined by spectroscopic methods and the in vitro antibacterial activity of newly synthesized compounds were carried out against some gram-positive and gram-negative bacteria by well diffusion method (zone inhibition). Our results have showed that these new synthesized compounds have much potent of antibacterial activity owing to containing of pyrazole and/or pyridazine, chromone, oxazine, furane, and pyrrole rings. Some of the new pyrazole derivatives exhibited higher activities than reference drugs against the representative bacteria.
Keywords:Pyrazole  Pyrazolo-pyridazine  Furandione  Oxazine  Pyrrole  Chromone  Antibacterial activity
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