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 journal › Journal article › Research › peer-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.
|Journal||Bioorganic & Medicinal Chemistry Letters|
|Number of pages||4|
|Publication status||Published - 15 Oct 2008|
- 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