SYNTHESIS AND PRELIMINARY PHARMACOLOGICAL EVALUATION OF 2-BENZYLOXY SUBSTITUTED ARYL KETONES AS 5-HT4 RECEPTOR ANTAGONISTS

被引：18

作者：

CLARK, RD

JAHANGIR, A

LANGSTON, JA

WEINHARDT, KK

MILLER, AB

LEUNG, E

BONHAUS, DW

WONG, EHF

EGLEN, RM

机构：

[1] SYNTEX INC,INST ANALYT RES,PALO ALTO,CA 94304

[2] SYNTEX INC,INST PHARMACOL,PALO ALTO,CA 94304

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(01)80414-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Structural modification of the 2-methoxy group and at the 4-position of the piperidine ring of the 5-HT4 partial agonist 1 led to analogues with increased affinity for the 5-HT4 receptor and loss of agonist activity. Similar modification of 2 resulted in 2-(3,5-dimethoxy)benzyloxy derivatives (23,24,26-28) that were found to be 5-HT4 receptor antagonists with subnanomolar affinity.

引用

页码：2481 / 2484

页数：4

共 7 条

[1]

BAXTER GS, 1991, N-S ARCH PHARMACOL, V343, P439

[2] KETONES RELATED TO THE BENZOATE 5-HT4 RECEPTOR ANTAGONIST RS-23597 ARE HIGH-AFFINITY PARTIAL AGONISTS [J].