Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties

被引：34

作者：

Bridges, Thomas M. ^{[1
,3
]}

Brady, Ashley E. ^{[1
,3
]}

Kennedy, J. Phillip ^{[2
]}

Daniels, R. Nathan ^{[2
]}

Miller, Nicole R. ^{[1
]}

Kim, Kwango ^{[3
]}

Breininger, Micah L. ^{[1
]}

Gentry, Patrick R. ^{[1
]}

Brogan, John T. ^{[2
]}

Jones, Carrie K. ^{[1
,3
]}

Conn, P. Jeffrey ^{[1
,3
]}

Lindsley, Craig W. ^{[1
,2
,3
]}

机构：

[1] Vanderbilt Univ, Med Ctr, Dept Pharmacol, Nashville, TN 37232 USA

[2] Vanderbilt Univ, Dept Chem, Nashville, TN 37232 USA

[3] Vanderbilt Inst Chem Biol, Vanderbilt Program Drug Discovery, Nashville, TN 37232 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 20期

关键词：

allosteric; agonist; TBPB; muscarinic receptor;

D O I：

10.1016/j.bmcl.2008.09.023

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This Letter describes the first account of the synthesis and SAR, developed through an iterative analogue library approach, of analogues of the highly selective M1 allosteric agonist TBPB. With slight structural changes, mAChR selectivity was maintained, but the degree of partial M1 agonism varied considerably. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：5439 / 5442

页数：4

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