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

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

Bioorganic & medicinal chemistry letters (2001-02-24)

C Zhou, L Guo, G Morriello, A Pasternak, Y Pan, S P Rohrer, E T Birzin, S E Huskey, T Jacks, K D Schleim, K Cheng, J M Schaeffer, A A Patchett, L Yang

PMID11212124

RÉSUMÉ

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).