N1-芳基磺酰基-3-(1,2,3,6-四氢吡啶-4-基)-1H-吲哚衍生物是强效且选择性的5-HT6受体拮抗剂。
N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists.
作者信息
Cole Derek C, Ellingboe John W, Lennox William J, Mazandarani Hossein, Smith Deborah L, Stock Joseph R, Zhang Guoming, Zhou Ping, Schechter Lee E
机构信息
Chemical and Screening Sciences, Wyeth Research, Pearl River, NY 10965, USA.
出版信息
Bioorg Med Chem Lett. 2005 Jan 17;15(2):379-83. doi: 10.1016/j.bmcl.2004.10.064.
A series of N(1)-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)indole derivatives was designed and synthesized. These compounds were shown to have high affinity for the 5-HT(6) receptor. Two analogs, 4-[3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole-1-sulfonyl]-phenylamine 15g and 4-[3-(1,2,3,6-tetrahydropyridin-4-yl)-5-methoxy-1H-indole-1-sulfonyl]-phenylamine 15y, had 0.4 and 3.0 nM affinity, respectively, and antagonized the production of adenylate cyclase at sub-nanomolar concentrations.
设计并合成了一系列N(1)-芳基磺酰基-3-(1,2,3,6-四氢吡啶-4-基)吲哚衍生物。这些化合物对5-HT(6)受体显示出高亲和力。两个类似物，4-[3-(1,2,3,6-四氢吡啶-4-基)-1H-吲哚-1-磺酰基]-苯胺15g和4-[3-(1,2,3,6-四氢吡啶-4-基)-5-甲氧基-1H-吲哚-1-磺酰基]-苯胺15y，分别具有0.4和3.0 nM的亲和力，并且在亚纳摩尔浓度下拮抗腺苷酸环化酶的产生。
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