Literature DB >> 19616429

Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists.

David G Washburn1, Tram H Hoang, James S Frazee, Latisha Johnson, Marlys Hammond, Sharada Manns, Kevin P Madauss, Shawn P Williams, Chaya Duraiswami, Thuy B Tran, Eugene L Stewart, Eugene T Grygielko, Lindsay E Glace, Walter Trizna, Rakesh Nagilla, Jeffrey D Bray, Scott K Thompson.   

Abstract

We have designed and synthesized a novel series of pyrrolidinones as progesterone receptor partial agonists. Compounds from this series had improved AR selectivity, rat pharmacokinetic properties, and in vivo potency compared to the lead compound. In addition, these compounds had improved selectivity against hERG channel inhibition.

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Year:  2009        PMID: 19616429     DOI: 10.1016/j.bmcl.2009.06.081

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


  3 in total

1.  Structural basis for agonism and antagonism for a set of chemically related progesterone receptor modulators.

Authors:  Scott J Lusher; Hans C A Raaijmakers; Diep Vu-Pham; Koen Dechering; Tsang Wai Lam; Angus R Brown; Niall M Hamilton; Olaf Nimz; Rolien Bosch; Ross McGuire; Arthur Oubrie; Jacob de Vlieg
Journal:  J Biol Chem       Date:  2011-08-17       Impact factor: 5.157

2.  Solid-phase synthesis of N-substituted pyrrolidinone-tethered N-substituted piperidines via Ugi reaction.

Authors:  Zhang Liu; Adel Nefzi
Journal:  J Comb Chem       Date:  2010-07-12

3.  Calcium(ii)-catalyzed enantioselective conjugate additions of amines.

Authors:  Brice E Uno; Rachel D Dicken; Louis R Redfern; Charlotte M Stern; Greg G Krzywicki; Karl A Scheidt
Journal:  Chem Sci       Date:  2018-01-10       Impact factor: 9.825

  3 in total

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