Monoamine Oxidase Inhibitory Activity of Novel Pyrazoline Analogues: Curcumin Based Design and Synthesis


Badavath V. N. , BAYSAL İ. , UÇAR G. , Sinha B. N. , Jayaprakash V.

ACS MEDICINAL CHEMISTRY LETTERS, cilt.7, ss.56-61, 2016 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 7 Konu: 1
  • Basım Tarihi: 2016
  • Doi Numarası: 10.1021/acsmedchemlett.5b00326
  • Dergi Adı: ACS MEDICINAL CHEMISTRY LETTERS
  • Sayfa Sayıları: ss.56-61

Özet

A series of new 2-methoxy-4-(5-pheny1-4,5dihydro-1H-pyrazol-3-yl)phenolderivatives, 4-13, were synthesized and tested for their human MAO inhibitory activity. All the compounds were found to be selective and reversible toward hMAO-A except 4, a selective inhibitor of hMAO-B and 12, a nonselective inhibitor. Compound 7 was found to be a potent inhibitor of hMAO-A with K-i = 0.06 +/- 0.003 mu M and was having selectivity index of (SI = 1.02 X 10(-5)). It was found to be better than standard drug, Moclobemide (hMAO-A with K = 0.11 +/- 0.01 mu M) with selectivity index of SI = 0.049. Molecular docking simulation was carried out to understand the crucial interactions responsible for selectivity and potency.