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Synthesis and biological characterization of a series of novel diaryl amide M₁ antagonists.

Abstract：

:Utilizing a combination of high-throughput and multi-step synthesis, SAR in a novel series of M(1) acetylcholine receptor antagonists was rapidly established. The efforts led to the discovery the highly potent M(1) antagonists 6 (VU0431263), and 8f (VU0433670). Functional Schild analysis and radioligand displacement experiments demonstrated the competitive, orthosteric binding of these compounds; human selectivity data are presented.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Poslusney MS,Sevel C,Utley TJ,Bridges TM,Morrison RD,Kett NR,Sheffler DJ,Niswender CM,Daniels JS,Conn PJ,Lindsley CW,Wood MR

doi

10.1016/j.bmcl.2012.09.011

subject

Has Abstract

pub_date

2012-11-15 00:00:00

pages

6923-8

issue

22

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)01155-9

journal_volume

22

pub_type

杂志文章

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