Inhibition of amine oxidases activity by 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives
2002; Elsevier BV; Volume: 12; Issue: 24 Linguagem: Inglês
10.1016/s0960-894x(02)00699-6
ISSN1464-3405
AutoresFedele Manna, Franco Chimenti, Adriana Bolasco, Daniela Secci, Bruna Bizzarri, Olivia Befani, Paola Turini, Bruno Mondovı̀, Stefano Alcaro, Andrea Tafi,
Tópico(s)Chemical Reactions and Mechanisms
ResumoA 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 I(50) 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.
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