Aryloxypyrazines as highly selective antagonists of Oxytocin.
A series of aryloxypyrazines were designed based on structural overlap with previously reported arylpyrazine Oxytocin antagonists. Similarly high levels of Oxytocin antagonism were achievable in this new series. In addition, significant improvements in selectivity over the related vasopressin V(1A) receptor were also possible.
Brown
Alan
A
Discovery Chemistry, Pfizer Global Research and Development, Sandwich, United Kingdom. Alan.D.Brown@pfizer.com
Ellis
Dave
D
Pearce
David
D
Ralph
Michael
M
Sciammetta
Nunzio
N
D065092:Antidiuretic Hormone Receptor Antagonists; D010121:Oxytocin / Q000037:antagonists & inhibitors*; D011719:Pyrazines / Q000138:chemical synthesis / Q000737:chemistry*
D065092:Antidiuretic Hormone Receptor Antagonists; D011719:Pyrazines; D010121:Oxytocin