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Bioorg Med Chem Lett. 2008 Oct 15;18(20):5443-7. doi: 10.1016/j.bmcl.2008.09.032. Epub 2008 Sep 11.

Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.

Author information

1
Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.

Abstract

This letter describes the further synthesis and SAR, developed through an iterative analog library approach, of analogs of the highly selective M1 allosteric agonist TBPB by deletion of the distal basic piperidine nitrogen by the formation of amides, sulfonamides and ureas. Despite the large change in basicity and topology, M1 selectivity was maintained.

PMID:
18829311
PMCID:
PMC3177607
DOI:
10.1016/j.bmcl.2008.09.032
[Indexed for MEDLINE]
Free PMC Article

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