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Piperidinyl-nicotinamides as potent and selective somatostatin receptor subtype 5 antagonists |
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| Authors: | André Alker Alfred Binggeli Andreas D Christ Luke Green Hans Peter Maerki Rainer E Martin Peter Mohr |
| Institution: | 1. F. Hoffmann-La Roche Ltd, Pharmaceuticals Division, Molecular Structure Research, CH-4070 Basel, Switzerland;2. F. Hoffmann-La Roche Ltd, Pharmaceuticals Division, Medicinal Chemistry, CH-4070 Basel, Switzerland;3. F. Hoffmann-La Roche Ltd, Pharmaceuticals Division, Discovery Metabolic & Vascular Diseases, CH-4070 Basel, Switzerland |
| Abstract: | 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 436 nM. 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 (R)-enantiomer. |
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