Design, synthesis, and in vitro hMAO-B inhibitory evaluation of some 1-methyl-3, 5-diphenyl-4, 5-dihydro-1H-pyrazoles
R Fioravanti, N Desideri, M Biava, LP Monaco… - Bioorganic & medicinal …, 2013 - Elsevier
R Fioravanti, N Desideri, M Biava, LP Monaco, L Grammatica, M Yáñez
Bioorganic & medicinal chemistry letters, 2013•ElsevierAbstract 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.
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.
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.
Elsevier
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