Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus

M S Kuo; M G Bock; R M Freidinger; M T Guidotti; E V Lis; J M Pawluczyk; D S Perlow; D J Pettibone; A G Quigley; D R Reiss; P D Williams; C J Woyden

doi:10.1016/S0960-894X(98)00568-X

Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus

Bioorg Med Chem Lett. 1998 Nov 3;8(21):3081-6. doi: 10.1016/S0960-894X(98)00568-X.

Authors

M S Kuo¹, M G Bock, R M Freidinger, M T Guidotti, E V Lis, J M Pawluczyk, D S Perlow, D J Pettibone, A G Quigley, D R Reiss, P D Williams, C J Woyden

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA.

PMID: 9873680
DOI: 10.1016/S0960-894X(98)00568-X

Abstract

Structure-activity studies on the oxytocin antagonist 1 (L-371,257) have identified a new series of high affinity, receptor-selective OT antagonists in which the N-acetyl-4-piperidinyl ether terminus in 1 has been replaced with a 1-(aryl)ethoxy group.

MeSH terms

Administration, Oral
Animals
Benzoxazines
Biological Availability
Female
Humans
Oxazines / pharmacology*
Oxytocin / antagonists & inhibitors*
Piperidines / pharmacology*
Rats
Structure-Activity Relationship

Substances

Benzoxazines
L 371257
Oxazines
Piperidines
Oxytocin