Design, synthesis, and in vitro hMAO-B inhibitory evaluation of some 1-methyl-3, 5-diphenyl-4, 5-dihydro-1H-pyrazoles

…, N Desideri, M Biava, LP Monaco, L Grammatica…

文献索引：Fioravanti, Rossella; Desideri, Nicoletta; Biava, Mariangela; Proietti Monaco, Luca; Grammatica, Laura; Yanez, Matilde Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 18 p. 5128 - 5130

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被引用次数: 11

摘要

Abstract A series of 1-methyl-3, 5-diphenyl-4, 5-dihydro-1H-pyrazoles (3a–k and 4a–u) were designed, synthesized, and evaluated for their inhibitory efficacy towards the two hMAO isoforms. Most of the derivatives were found to be potent and selective hMAO-B inhibitors. In particular, derivative 3g showed greater hMAO-B affinity than selective inhibitor selegiline coupled with high selectivity index (SI= 145). The most selective hMAO-B inhibitor was the ...