Title of article
Synthesis and structure–activity relationships of thieno[2,3-b]pyrroles as antagonists of the GnRH receptor
Author/Authors
Jean Claude Arnould، نويسنده , , Bénédicte Delouvrié، نويسنده , , Pascal Boutron، نويسنده , , Al G. Dossetter، نويسنده , , Kevin M. Foote، نويسنده , , Annie Hamon، نويسنده , , Urs Hancox، نويسنده , , Craig S. Harris، نويسنده , , Mike Hutton، نويسنده , , Maryannick Lamorlette، نويسنده , , Zbigniew Matusiak، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
7
From page
6448
To page
6454
Abstract
A new class of small-molecule GnRH antagonists, the thieno[2,3-b]pyrroles, was designed. Herein, the synthesis and structure–activity relationships are described. Substitution at the C4 position was investigated; during this study, it was observed that introducing piperazines and piperidines improved the physical properties of the compounds while retaining good in vitro potency. This exploration led to the discovery of amidopiperidines with improved pharmacokinetic properties.
Keywords
GNRH , receptor , Antagonist , 3-b]pyrrole , LHRH
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798822
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