Identification of potent and selective oxytocin antagonists. Part 1: indole and benzofuran derivatives.
Studies to discover novel, potent and selective oxytocin antagonists are reported. Combinatorial libraries designed to find novel replacements of fragments of oxytocin antagonist L-371,257, identified pyrimidine, thiazole, indole and benzofuran as potential alternatives to the benzoic acid moiety of L-371,257. Additional investigations identified indole and benzofuran derivatives with potent oxytocin antagonist activity.
Wyatt
Paul G
PG
Department of Medicinal Chemistry, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, SG1 2NY, Herts, UK.
Allen
Michael J
MJ
Chilcott
Josie
J
Foster
Alison
A
Livermore
David G
DG
Mordaunt
Jackie E
JE
Scicinski
Jan
J
Woollard
Patrick M
PM
D000818:Animals; D001572:Benzofurans / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D001682:Biological Availability; D004285:Dogs; D015195:Drug Design; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D010121:Oxytocin / Q000037:antagonists & inhibitors*; D018045:Receptors, Oxytocin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D001572:Benzofurans; D007211:Indoles; D018045:Receptors, Oxytocin; D010121:Oxytocin