Literature DB >> 18805692

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

Thomas M Bridges1, Ashley E Brady, J Phillip Kennedy, R Nathan Daniels, Nicole R Miller, Kwango Kim, Micah L Breininger, Patrick R Gentry, John T Brogan, Carrie K Jones, P Jeffrey Conn, Craig W Lindsley.   

Abstract

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.

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Year:  2008        PMID： 18805692      PMCID： PMC3177598          DOI： 10.1016/j.bmcl.2008.09.023

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


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