e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521
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
…, TM Bridges, AE Brady, PJ Conn, CW Lindsley
Index: Miller, Nicole R.; Daniels, R. Nathan; Bridges, Thomas M.; Brady, Ashley E.; Conn, P. Jeffrey; Lindsley, Craig W. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 20 p. 5443 - 5447
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.
