Design,synthesis, and in vitro hMAO-B inhibitory evaluation of some 1-methyl-3,5-diphenyl-4,5-dihydro-1H-pyrazoles |
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| Authors: | Rossella Fioravanti Nicoletta Desideri Mariangela Biava Luca Proietti Monaco Laura Grammatica Matilde Yáñez |
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| Institution: | 1. Dipartimento di Chimica e Tecnologie del Farmaco, Università ‘La Sapienza’ P.le Aldo Moro 5, 00185 Rome, Italy;2. Departamento de Farmacología and Instituto de Farmacia Industrial, Facultad de Farmacia, Universidad de Santiago de Compostela, Campus Universitario Sur, E-15782 Santiago de Compostela, La Coruña, Spain |
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| 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 3-methyl analogue 3f with an SI higher than 909. |
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| Keywords: | Pyrazole derivatives Monoamine oxidases hMAO inhibitors |
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