A study on synthesis and antimicrobial activity of 4-acyl-pyrazoles


Cetin A., Bildirici İ.

JOURNAL OF SAUDI CHEMICAL SOCIETY, cilt.22, sa.3, ss.279-296, 2018 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 22 Sayı: 3
  • Basım Tarihi: 2018
  • Doi Numarası: 10.1016/j.jscs.2016.05.008
  • Dergi Adı: JOURNAL OF SAUDI CHEMICAL SOCIETY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.279-296
  • Anahtar Kelimeler: Pyrazole, Pyrazolo-pyridazine, Furandione, Oxazine, Pyrrole, Chromone, Antibacterial activity, CYCLIC OXALYL COMPOUNDS, PYRAZOLE DERIVATIVES, BIOLOGICAL EVALUATION, INHIBITORS, ANTIBACTERIAL, DESIGN, ACID, HYBRIDS
  • Van Yüzüncü Yıl Üniversitesi Adresli: Evet

Özet

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. (C) 2016 King Saud University. Production and hosting by Elsevier B.V.