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.

Manna, F., Chimenti, F., Bolasco, A., Secci, D., Bizzarri, B., Befani, B., et al. (2002). Inhibition of Amine Oxidases Activity by 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-Pyrazole Derivatives. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 12(24), 3629-3633 [10.1016/S0960-894X(02)00699-6].

Inhibition of Amine Oxidases Activity by 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-Pyrazole Derivatives

TAFI, ANDREA
2002

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.
Manna, F., Chimenti, F., Bolasco, A., Secci, D., Bizzarri, B., Befani, B., et al. (2002). Inhibition of Amine Oxidases Activity by 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-Pyrazole Derivatives. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 12(24), 3629-3633 [10.1016/S0960-894X(02)00699-6].
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11365/40622
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