基于吡唑啉的 MAO 抑制剂：合成、生物评价和 SAR 研究。
Pyrazoline based MAO inhibitors: synthesis, biological evaluation and SAR studies.
机构信息
Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi 835215, Jharkhand, India.
出版信息
Bioorg Med Chem Lett. 2011 Jul 15;21(14):4296-300. doi: 10.1016/j.bmcl.2011.05.057. Epub 2011 May 25.
Twenty-two pyrazoline derivatives were synthesized and tested for their human MAO (hMAO) inhibitory activity. Twelve molecules with unsubstituted ring A and substituted ring C (5-16) were found to be potent inhibitors of hMAO-A isoform with SI(MAO-A) in the order 10(3) and 10(4). Ten molecules with unsubstituted ring A and without ring C (21-30), in which eight molecules (21, 23-26, and 28-30) were selective for hMAO-A, one for hMAO-B (22) and the other one non-selective (27). Presence of ring C increases potency as well as SI towards hMAO-A; however its absence decreases both potency and SI towards hMAO-A and hMAO-B.
合成了 22 种吡唑啉衍生物，并测试了它们对人单胺氧化酶（hMAO）的抑制活性。12 种 A 环未取代且 C 环取代的分子（5-16）对 hMAO-A 同工酶表现出很强的抑制活性，SI（MAO-A）值在 10（3）到 10（4）之间。10 种 A 环未取代且无 C 环的分子（21-30）中，有 8 种分子（21、23-26 和 28-30）对 hMAO-A 具有选择性，1 种对 hMAO-B（22）具有选择性，另 1 种是非选择性的（27）。C 环的存在增加了对 hMAO-A 的活性和选择性指数；然而，它的缺失降低了对 hMAO-A 和 hMAO-B 的活性和选择性指数。
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