Synthesis and structure activity relationship of guanidines as NPY Y5 antagonists

Christopher J Aquino; Joshi M Ramanjulu; Dennis Heyer; Alejandro J Daniels; Fabio Palazzo; Milana Dezube

doi:10.1016/j.bmc.2004.03.012

Synthesis and structure activity relationship of guanidines as NPY Y5 antagonists

Bioorg Med Chem. 2004 May 15;12(10):2691-708. doi: 10.1016/j.bmc.2004.03.012.

Authors

Christopher J Aquino¹, Joshi M Ramanjulu, Dennis Heyer, Alejandro J Daniels, Fabio Palazzo, Milana Dezube

Affiliation

¹ Department of Medicinal Chemistry, GlaxoSmithKline, RTP, NC 27709, USA. [email protected]

PMID: 15110851
DOI: 10.1016/j.bmc.2004.03.012

Abstract

A series of bis-aryl substituted guanidines have been discovered as potent NPY Y5 antagonists. The SAR and in vitro metabolic stability of these compounds are discussed.

MeSH terms

Animals
CHO Cells
Cricetinae
Cricetulus
Guanidines / chemical synthesis*
Guanidines / chemistry
Guanidines / pharmacology*
Molecular Structure
Radioligand Assay
Receptors, Neuropeptide Y / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Guanidines
Receptors, Neuropeptide Y
neuropeptide Y5 receptor