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.
Dordal
Alberto
A
Laboratorios Dr Esteve S.A. Av.Mare de Déu de Montserrat, Barcelona, Spain.
Lipkin
Mike
M
Macritchie
Jackie
J
Mas
Josep
J
Port
Adriana
A
Rose
Sally
S
Salgado
Leonardo
L
Savic
Vladimir
V
Schmidt
Wolfgang
W
Serafini
Maria Teresa
MT
Spearing
William
W
Torrens
Antoni
A
Yeste
Sandra
S
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