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Synthesis and SAR of amino acid-derived heterocyclic progesterone receptor full and partial agonists.
Hammond, Marlys; Patterson, Jaclyn R; Manns, Sharada; Hoang, Tram H; Washburn, David G; Trizna, Walter; Glace, Lindsay; Grygielko, Eugene T; Nagilla, Rakesh; Nord, Melanie; Fries, Harvey E; Minick, Douglas J; Laping, Nicholas J; Bray, Jeffrey D; Thompson, Scott K.
Affiliation
  • Hammond M; Department of Chemistry, Metabolic Pathways Centre for Excellence in Drug Discovery, GlaxoSmithKline Pharmaceuticals, King of Prussia, PA, USA. marlys.2.hammond@gsk.com
Bioorg Med Chem Lett ; 19(10): 2637-41, 2009 May 15.
Article in En | MEDLINE | ID: mdl-19376703
ABSTRACT
Two classes of amino acid-derived heterocyclic progesterone receptor ligands were developed to address the metabolic issues posed by the dimethyl amide functionality of the lead compound (1). The tetrazole-derived ligands behaved as potent partial agonists, while the 1,2,4-triazole ligands behaved as potent full agonists.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Tetrazoles / Receptors, Progesterone Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2009 Document type: Article Affiliation country:
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Tetrazoles / Receptors, Progesterone Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2009 Document type: Article Affiliation country: