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

Bridges TM, Brady AE, Kennedy JP, Daniels RN, Miller NR, Kim K, Breininger ML, Gentry PR, Brogan JT, Jones CK, Conn PJ, Lindsley CW
Bioorg Med Chem Lett. 2008 18 (20): 5439-42

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

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.

MeSH Terms (16)

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

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