Inhibitors of phenylethanolamine N-methyltransferase devoid of α2-adrenoceptor affinity
Inhibitors of phenylethanolamine N-methyltransferase devoid of α2-adrenoceptor affinity
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DOI：
10.1016/j.bmcl.2005.08.033
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发表时间：
2005-12-01
影响因子：
2.7
通讯作者：
Moro, CO
中科院分区：
文献类型：
--
作者：
Grunewald, GL;Lu, J;Moro, CO
合成了一系列 3-三氟甲基-1,2,3,4-四氢异喹啉，并评估了它们的苯乙醇胺 N-甲基转移酶 (PNMT) 抑制效力和对 α(2)-肾上腺素受体的亲和力。尽管与相应的 3-甲基-、3-羟甲基-或 3-未取代-THIQ 相比，它们的 PNMT 抑制效力有所下降，但其中一些由于其极低的 α2-肾上腺素受体亲和力而表现出良好的选择性。 (c) 2005 Elsevier Ltd. 保留所有权利。
A series of 3-trifluoromethyl-1,2,3,4-tetrahydroisoquinolines was synthesized and evaluated for their phenylethanolamine N-methyltransferase (PNMT) inhibitory potency and affinity for the alpha(2)-adrenoceptor. Although their PNMT inhibitory potency decreased compared with corresponding 3-methyl-, 3-hydroxymethyl- or 3-unsubstituted-THIQs, some of them showed good selectivity due to their extremely low a2-adrenoceptor affinity. (c) 2005 Elsevier Ltd. All rights reserved.