Inhibition of amine oxidases activity by 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives
| Autor: | Bruna Bizzarri, Paola Turini, Stefano Alcaro, Olivia Befani, Andrea Tafi, Fedele Manna, Bruno Mondovi, Daniela Secci, Franco Chimenti, Adriana Bolasco |
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| Rok vydání: | 2002 |
| Předmět: |
Models
Molecular Amine oxidase Monoamine Oxidase Inhibitors Swine medicine.drug_class Stereochemistry Clinical Biochemistry Pharmaceutical Science Pyrazole Biochemistry Substrate Specificity Structure-Activity Relationship chemistry.chemical_compound Non-competitive inhibition Drug Discovery medicine Animals Bovine serum albumin Monoamine Oxidase Molecular Biology Monoamine oxidase inhibitor Oxidase test biology Organic Chemistry General Medicine Monoamine neurotransmitter chemistry biology.protein Pyrazoles Molecular Medicine Cattle Amine gas treating Amine Oxidase (Copper-Containing) Monoamine oxidase B |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 12:3629-3633 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(02)00699-6 |
| Popis: | 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 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. |
| Databáze: | OpenAIRE |
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