Design and optimization of potent, selective antagonists of Oxytocin.
A novel series of Oxytocin antagonists are described. This series was identified through pharmacophoric overlap of in-house and literature antagonists. Subsequent optimization led to a series of potent, selective antagonists. Several analogues displayed oral bioavailability in vivo in the rat.
Brown
Alan
A
Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. Alan.D.Brown@pfizer.com
Brown
Lindsay
L
Ellis
Dave
D
Puhalo
Nicholas
N
Smith
Chris R
CR
Wallace
Olga
O
Watson
Lesa
L
D000284:Administration, Oral; D000818:Animals; D020650:Combinatorial Chemistry Techniques; D015394:Molecular Structure; D010120:Oxytocics / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D010121:Oxytocin / Q000037:antagonists & inhibitors*; D051381:Rats; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*
D010120:Oxytocics; D014230:Triazoles; D010121:Oxytocin