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

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

doi:10.1016/s0960-894x(00)00687-9

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

Bioorg Med Chem Lett. 2001 Feb 12;11(3):415-7. doi: 10.1016/s0960-894x(00)00687-9.

Authors

C Zhou¹, 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

Affiliation

¹ Merck Research Laboratories, Rahway, NJ 07065, USA. [email protected]

PMID: 11212124
DOI: 10.1016/s0960-894x(00)00687-9

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).

MeSH terms

Animals
Combinatorial Chemistry Techniques
Humans
Isomerism
Nipecotic Acids / chemical synthesis
Nipecotic Acids / metabolism*
Oligopeptides / chemical synthesis
Oligopeptides / metabolism
Protein Binding
Receptors, Somatostatin / agonists*
Receptors, Somatostatin / metabolism
Structure-Activity Relationship

Substances

Nipecotic Acids
Oligopeptides
Receptors, Somatostatin
nipecotic acid amide
somatostatin receptor 5
somatostatin receptor 2