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Bioorganic & medicinal chemistry letters

Nipecotic and iso-nipecotic amides as potent and selective somatostatin subtype-2 receptor agonists.


PMID 11212124

Abstract

N-Substituted nipecotic and iso-nipecotic amides of beta-methylTrpLys tert-butyl ester were found to be novel, selective and potent agonists of the somatostatin subtype-2 receptor in vitro. For example iso-nipecotic amide 8a showed high hsst2 binding affinity (Ki = 0.5 nM) and good selectivity (h5/h2 = 832).

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