Discovery and SAR of cyclic isothioureas as novel NPY Y1 receptor antagonists.
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.
Department of Medicinal Chemistry, Schering Plough Research Institute, Kenilworth, NJ 07033, USA. zhong-yue.sun@spcorp.com
Zhong-Yue
ZY
Sun
Zhaoning
Z
Zhu
Yuanzan
Y
Ye
Brian
B
McKittrick
Michael
M
Czarniecki
William
W
Greenlee
Deborra
D
Mullins
Mario
M
Guzzi
D003500:Cyclization; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D008024:Ligands; D015394:Molecular Structure; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013890:Thiourea / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*
D008024:Ligands; D017476:Receptors, Neuropeptide Y; C097212:neuropeptide Y-Y1 receptor; D013890:Thiourea