1.
Bioorg Med Chem Lett
; 22(14): 4849-53, 2012 Jul 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-22683222
RESUMO
Further application of our multivalent approach to drug discovery directed to 5-HT(4) receptor agonists is described. Optimization of the linker and secondary binding amine in the indazole-tropane primary binding group series, for binding affinity and functional potency at the 5-HT(4) receptor, selectivity over the 5-HT(3) receptor, oral pharmacokinetics, and in vivo efficacy in models of GI motility, resulted in the identification of clinical compound TD-2749.