e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521
Synthesis and structure-activity relationships of potent and orally active 5-HT4 receptor antagonists: indazole and benzimidazolone derivatives
…, AD Susemichel, DO Calligaro, ML Cohen
Index: Schaus, John M.; Thompson, Dennis C.; Bloomquist, William E.; Susemichel, Alice D.; Calligaro, David O.; Cohen, Marlene L. Journal of Medicinal Chemistry, 1998 , vol. 41, # 11 p. 1943 - 1955
A series of indole-3-carboxamides, indazole-3-carboxamides, and benzimidazolone-3- carboxamides was synthesized and evaluated for antagonist affinity at the 5-HT4 receptor in the rat esophagus. The endo-3-tropanamine derivatives in the indazole and benzimidazolone series possessed greater 5-HT4 receptor affinity than the corresponding indole analogues. 5-HT4 receptor antagonist affinity was further increased by alkylation at ...
