Piperidinyl-nicotinamides as potent and selective somatostatin receptor subtype 5 antagonists

…, A Binggeli, AD Christ, L Green, HP Maerki…

文献索引：Alker, Andre; Binggeli, Alfred; Christ, Andreas D.; Green, Luke; Maerki, Hans Peter; Martin, Rainer E.; Mohr, Peter Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 15 p. 4521 - 4525

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被引用次数: 3

摘要

Nicotinamides of benzyl-substituted 4-aminopiperidines and their seven-membered analogs of generic structure 2 and 2′ have been discovered as potent and selective SST5 antagonists. The activity (Ki) ranges from 2.4 to 436nM. Most compounds exhibit decent physicochemical properties and follow a clear SAR pattern. Interestingly enough, the receptor is strongly enantiodiscriminating and binds in the amino-azepane-series only the ...