Discovery and SAR of cyclic isothioureas as novel NPY Y1 receptor antagonists

Zhong-Yue Sun; Zhaoning Zhu; Yuanzan Ye; Brian McKittrick; Michael Czarniecki; William Greenlee; Deborra Mullins; Mario Guzzi

doi:10.1016/j.bmcl.2009.09.048

Discovery and SAR of cyclic isothioureas as novel NPY Y1 receptor antagonists

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6801-5. doi: 10.1016/j.bmcl.2009.09.048. Epub 2009 Sep 25.

Authors

Zhong-Yue Sun¹, Zhaoning Zhu, Yuanzan Ye, Brian McKittrick, Michael Czarniecki, William Greenlee, Deborra Mullins, Mario Guzzi

Affiliation

¹ Department of Medicinal Chemistry, Schering Plough Research Institute, Kenilworth, NJ 07033, USA. [email protected]

PMID: 19864135
DOI: 10.1016/j.bmcl.2009.09.048

Abstract

A class of novel 2-aminobenzothiazoles have been identified as NPY Y(1) antagonists. Various N-heterocyclic substituted aminophenethyl-2-aminobenzothiazole analogs were synthesized to explore the SAR. Isothiourea analogs and ligands with high potency (K(i) 30 nM) have been identified.

MeSH terms

Cyclization
Dose-Response Relationship, Drug
Drug Discovery*
Ligands
Molecular Structure
Receptors, Neuropeptide Y / antagonists & inhibitors*
Stereoisomerism
Structure-Activity Relationship
Thiourea / analogs & derivatives
Thiourea / chemistry
Thiourea / pharmacology*

Substances

Ligands
Receptors, Neuropeptide Y
neuropeptide Y-Y1 receptor
Thiourea