Identification of potent and selective oxytocin antagonists. Part 1: indole and benzofuran derivatives

Paul G. Wyatt; Michael J. Allen; Josie Chilcott; Alison Foster; David G. Livermore; Jackie E. Mordaunt; Jan Scicinski; Patrick M. Woollard

doi:10.1016/S0960-894X(02)00159-2

Identification of potent and selective oxytocin antagonists. Part 1: indole and benzofuran derivatives

Paul G. Wyatt, Michael J. Allen, Josie Chilcott, Alison Foster, David G. Livermore, Jackie E. Mordaunt, Jan Scicinski, Patrick M. Woollard

Research output: Contribution to journal › Article › peer-review

37 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	1399-404
Number of pages	6
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	12
Issue number	10
Early online date	22 Mar 2002
DOIs	https://doi.org/10.1016/S0960-894X(02)00159-2
Publication status	Published - 20 May 2002

Keywords

Animals
Benzofurans
Biological Availability
Dogs
Drug Design
Humans
Indoles
Kinetics
Models, Molecular
Molecular Conformation
Oxytocin
Receptors, Oxytocin
Structure-Activity Relationship

Access to Document

10.1016/S0960-894X(02)00159-2

Cite this

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title = "Identification of potent and selective oxytocin antagonists. Part 1: indole and benzofuran derivatives",

abstract = "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.",

keywords = "Animals, Benzofurans, Biological Availability, Dogs, Drug Design, Humans, Indoles, Kinetics, Models, Molecular, Molecular Conformation, Oxytocin, Receptors, Oxytocin, Structure-Activity Relationship",

author = "Wyatt, {Paul G.} and Allen, {Michael J.} and Josie Chilcott and Alison Foster and Livermore, {David G.} and Mordaunt, {Jackie E.} and Jan Scicinski and Woollard, {Patrick M.}",

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AU - Wyatt, Paul G.

AU - Allen, Michael J.

AU - Chilcott, Josie

AU - Foster, Alison

AU - Livermore, David G.

AU - Mordaunt, Jackie E.

AU - Scicinski, Jan

AU - Woollard, Patrick M.

PY - 2002/5/20

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AB - 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.

KW - Animals

KW - Benzofurans

KW - Biological Availability

KW - Dogs

KW - Drug Design

KW - Humans

KW - Indoles

KW - Kinetics

KW - Models, Molecular

KW - Molecular Conformation

KW - Oxytocin

KW - Receptors, Oxytocin

KW - Structure-Activity Relationship

U2 - 10.1016/S0960-894X(02)00159-2

DO - 10.1016/S0960-894X(02)00159-2

M3 - Article

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VL - 12

SP - 1399

EP - 1404

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

SN - 0960-894X

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ER -