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.
Sun
Zhong-Yue
ZY
Department of Medicinal Chemistry, Schering Plough Research Institute, Kenilworth, NJ 07033, USA. zhong-yue.sun@spcorp.com
Zhu
Zhaoning
Z
Ye
Yuanzan
Y
McKittrick
Brian
B
Czarniecki
Michael
M
Greenlee
William
W
Mullins
Deborra
D
Guzzi
Mario
M
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