Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/4657
Title: Inhibition of Amine Oxidases Activity by 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-Pyrazole Derivatives
Authors: Manna, F.
Chimenti, F.
Bolasco, A.
Secci, D.
Bizzarri, B.
Befani, B.
Turini, P.
Mondovì, B.
Alcaro, S.
Tafi, Andrea 
Issue Date: 2002
Project: None 
Journal: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Abstract: 
A novel series of 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives have been synthesised and investigated for the ability to inhibit selectively monoamine oxidases, swine kidney oxidase, and bovine serum amine oxidase. The newly synthesised compounds 1-6 proved to be reversible and non-competitive inhibitors of all types of the assayed amine oxidases. Compounds inhibit monoamine oxidases potently, displaying low 150 values of particular interest. In particular 1-acetyl-3-(2,4-dihydroxyphenyl)-5-(3-methylphenyl)-4,5-dihydro-(1H)-pyrazole 6 showed to be a potent monoamine oxidase inhibitor with a K-i of about 10(-8) M. Further insights in the theoretical evaluation of the possible interactions between the compounds and monoamine oxidase B have been developed through a computational approach. (C) 2002 Elsevier Science Ltd. All rights reserved.
Description: 
19464
URI: http://hdl.handle.net/20.500.12779/4657
ISSN: 0960-894X
DOI: 10.1016/S0960-894X(02)00699-6
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