A preliminary study of the metabolic stability of a series of benzoxazinone derivatives as potent neuropeptide Y5 antagonists.
The metabolic stability of benzoxazinone derivatives, a potent series of NPY Y5 antagonists, has been investigated. This study resulted in the identification of the structural moieties prone to metabolic transformations and which strongly influenced the in vitro half-life. This provides opportunities to optimize the structure of this new class of NPY Y5 antagonists.
Laboratorios Dr Esteve S.A. Av.Mare de Déu de Montserrat, Barcelona, Spain.
Alberto
A
Dordal
Mike
M
Lipkin
Jackie
J
Macritchie
Josep
J
Mas
Adriana
A
Port
Sally
S
Rose
Leonardo
L
Salgado
Vladimir
V
Savic
Wolfgang
W
Schmidt
Maria Teresa
MT
Serafini
William
W
Spearing
Antoni
A
Torrens
Sandra
S
Yeste
D004353:Drug Evaluation, Preclinical; D004355:Drug Stability; D015394:Molecular Structure; D010078:Oxazines / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
D010078:Oxazines; D017476:Receptors, Neuropeptide Y; C100568:neuropeptide Y5 receptor