Literature DB >> 19376703

Synthesis and SAR of amino acid-derived heterocyclic progesterone receptor full and partial agonists.

Marlys Hammond1, Jaclyn R Patterson, Sharada Manns, Tram H Hoang, David G Washburn, Walter Trizna, Lindsay Glace, Eugene T Grygielko, Rakesh Nagilla, Melanie Nord, Harvey E Fries, Douglas J Minick, Nicholas J Laping, Jeffrey D Bray, Scott K Thompson.   

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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Year:  2009        PMID: 19376703     DOI: 10.1016/j.bmcl.2009.03.146

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  Chemistry and biology of multicomponent reactions.

Authors:  Alexander Dömling; Wei Wang; Kan Wang
Journal:  Chem Rev       Date:  2012-03-22       Impact factor: 60.622

2.  Development of a Method for the N-Arylation of Amino Acid Esters with Aryl Triflates.

Authors:  Sandra M King; Stephen L Buchwald
Journal:  Org Lett       Date:  2016-08-08       Impact factor: 6.005

  2 in total

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