Literature DB >> 18829311

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.

Nicole R Miller1, R Nathan Daniels, Thomas M Bridges, Ashley E Brady, P Jeffrey Conn, Craig W Lindsley.   

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.

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Year:  2008        PMID： 18829311      PMCID： PMC3177607          DOI： 10.1016/j.bmcl.2008.09.032

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


  14 in total

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7.  Identification of a family of muscarinic acetylcholine receptor genes.

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9.  Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity.

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Review 10.  Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders.

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