Synthesis and structure activity relationship of guanidines as NPY Y5 antagonists.
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.
Aquino
Christopher J
CJ
Department of Medicinal Chemistry, GlaxoSmithKline, RTP, NC 27709, USA. cja9377@gsk.com
Ramanjulu
Joshi M
JM
Heyer
Dennis
D
Daniels
Alejandro J
AJ
Palazzo
Fabio
F
Dezube
Milana
M
D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D006146:Guanidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D011869:Radioligand Assay; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D006146:Guanidines; D017476:Receptors, Neuropeptide Y; C100568:neuropeptide Y5 receptor