Synthesis and structure–activity relationships of thieno[2,3-b]pyrroles as antagonists of the GnRH receptor
Bioorganic & Medicinal Chemistry Letters（2007）
Abstract
The synthesis and structure–activity relationships (SAR) of GnRH receptor antagonists based on thieno[2,3-b]pyrrole scaffold are described. Introduction of a piperidine moiety at C4 position led to compounds combining good in vitro potency and improved pharmacokinetics.
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Key words
GnRH,Receptor,Antagonist,Thieno[2,3-b]pyrrole,LHRH
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