New generation dopaminergic agents 4. Exploiting the 2-methyl chroman scaffold. Synthesis and evaluation of two novel series of 2-(aminomethyl)-3,4,7,9-tetrahydro-2H-pyrano[2,3-e]indole and indol-8-one derivatives

被引:14
|
作者
Mewshaw, RE
Marquis, KL
Shi, XJ
McGaughey, G
Stack, G
Webb, MB
Abou-Gharbia, M
Wasik, T
Scerni, R
Spangler, T
Brennan, JA
Mazandarani, H
Coupet, J
Andree, TH
机构
[1] Wyeth Ayerst Res Labs, Dept Chem Sci, Princeton, NJ 08543 USA
[2] Wyeth Ayerst Res Labs, CNS Disorders Dept, Princeton, NJ 08543 USA
关键词
D O I
10.1016/S0040-4020(98)00349-4
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The rational design, synthesis, and evaluation of two novel series of 2-(aminomethyl)-3,4,7,9-tetrahydro-2H-pyrano[2,3-e]indole and indolone derivatives rue disclosed, based on the recently discovered D-2 agonist phenolic template prototype [i.e. the 7-OH-2-(aminomethyl)chroman nucleus]. The indolones were observed to have higher affinity and intrinsic activity than the corresponding indoles. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:7081 / 7108
页数:28
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