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

Bioorganic & medicinal chemistry letters ·Vol. 11 ·No. 3 ·2001-02-12 ·Pages 415-7

Zhou C, Guo L, Morriello G, Pasternak A, Pan Y, Rohrer SP, Birzin ET, Huskey SE, Jacks T, Schleim KD, Cheng K, Schaeffer JM, Patchett AA, Yang L

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,metabolism Oligopeptides/chemical synthesis,metabolism Protein Binding Receptors, Somatostatin/agonists,metabolism Structure-Activity Relationship

Chemicals

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

Authors & Affiliations

14 authors, click to expand affiliations / ORCID

Zhou C

Merck Research Laboratories, Rahway, NJ 07065, USA. changyou_zhou@merck.com

Guo L

Morriello G

Pasternak A

Pan Y

Rohrer S P

Birzin E T

Huskey S E

Jacks T

Schleim K D

Cheng K

Schaeffer J M

Patchett A A

Yang L

Article Info

Journal

Bioorganic & medicinal chemistry letters

Abbr.

Bioorg Med Chem Lett

ISSN

0960-894X

DOI

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

changyou_zhou@merck.com

Published

2001-02-12

Pages

415-7

Language

English

Region

England

NLM ID

9107377

Subset

External Links

PubMed source DOI: 10.1016/s0960-894x(00)00687-9 View journal details

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

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