Dipartimento di Chimica e Tecnologie del Farmaco, Università La Sapienza, Rome, Italy.
Bioorg Med Chem Lett. 2013 Sep 15;23(18):5128-30. doi: 10.1016/j.bmcl.2013.07.035. Epub 2013 Jul 23.
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.
设计、合成了一系列 1-甲基-3,5-二苯基-4,5-二氢-1H-吡唑（3a-k 和 4a-u），并评估了它们对两种 hMAO 同工酶的抑制效果。大多数衍生物被发现是有效的和选择性的 hMAO-B 抑制剂。特别是，衍生物 3g 显示出比选择性抑制剂司来吉兰更强的 hMAO-B 亲和力，并且具有高选择性指数（SI=145）。最具选择性的 hMAO-B 抑制剂是 3-甲基类似物 3f，其 SI 高于 909。
