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  • Title: Synthesis, molecular modeling studies and selective inhibitory activity against MAO of N1-propanoyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives.
    Author: Chimenti F, Fioravanti R, Bolasco A, Manna F, Chimenti P, Secci D, Rossi F, Turini P, Ortuso F, Alcaro S, Cardia MC.
    Journal: Eur J Med Chem; 2008 Oct; 43(10):2262-7. PubMed ID: 18281126.
    Abstract:
    A series of N1-propanoyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives were synthesized and assayed as inhibitors of MAO-A and MAO-B isoforms. Most of the tested compounds showed inhibitory activity with micromolar values and MAO-A selectivity. In addition a computational work was carried out on the most selective compound 3b to highlight the most relevant interactions in the mechanism of recognition within both the MAO-A and the MAO-B enzyme active sites.
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