Substituted benzamides with conformationally restricted side chains. 5. Azabicyclo [xyz] derivatives as 5-HT4 receptor agonists and gastric motility stimulants

FD King, MS Hadley, KT Joiner, RT Martin…

文献索引：King, Frank D.; Hadley, Michael S.; Joiner, Karen T.; Martin, Roger T.; Sanger, Gareth J.; et al. Journal of Medicinal Chemistry, 1993 , vol. 36, # 6 p. 683 - 689

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被引用次数: 55

摘要

The syntheses of benzamides containing azabicyclo [xy zl side chains and their 5-HT4 receptor agonist and 5-HT3 receptor antagonist properties are described. These compounds were designed to mimic higher energy conformations of quinolizidine and indolizidine. High potency was achieved for both activities although an exactly paralleling SAR was not apparent. Introduction of 0 and S resulted in only marginal differences in potency which ...