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

Research output: Contribution to journalJournal articleResearchpeer-review

Thomas M Bridges, 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

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.

Original languageEnglish
JournalBioorganic & Medicinal Chemistry Letters
Volume18
Issue number20
Pages (from-to)5439-42
Number of pages4
ISSN0960-894X
DOIs
Publication statusPublished - 15 Oct 2008
Externally publishedYes

    Research areas

  • Acetylcholine/chemistry, Allosteric Regulation, Allosteric Site, Benzimidazoles/chemical synthesis, Binding Sites, Chemistry, Pharmaceutical/methods, Dose-Response Relationship, Drug, Drug Design, Humans, Inhibitory Concentration 50, Ligands, Models, Chemical, Piperidines/chemical synthesis, Receptor, Muscarinic M1/chemistry, Structure-Activity Relationship, Time Factors

ID: 213627759