Journal of Medicinal Chemistry 1992-10-16

Orally active, nonpeptide oxytocin antagonists.

B E Evans, J L Leighton, K E Rittle, K F Gilbert, G F Lundell, N P Gould, D W Hobbs, R M DiPardo, D F Veber, D J Pettibone

Index: J. Med. Chem. 35 , 3919, (1992)

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Abstract

The first nonpeptide antagonists of the neurohypophyseal hormone, oxytocin (OT) are described. Derivatives of the spiroindenepiperidine ring system, these compounds include L-366,509, an orally bioavailable OT antagonist with good in vivo duration. The potential use of these agents for treatment of preterm labor and their significance as new nonpeptide ligands for peptide receptors are discussed.