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

来源：

TETRAHEDRON | 1998年 / 54卷 / 25期

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

页码：7081 / 7108

页数：28

共 30 条

[1] DRUG DESIGN VIA PHARMACOPHORE IDENTIFICATION - DOPAMINERGIC ACTIVITY OF 3H-BENZ[E]INDOL-8-AMINES AND THEIR MODE OF INTERACTION WITH THE DOPAMINE RECEPTOR [J].