Literature DB >> 17070062

Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder.

David C Pryde1, Andrew S Cook, Denise J Burring, Lyn H Jones, Stephanie Foll, Michelle Y Platts, Vivienne Sanderson, Martin Corless, Alan Stobie, Donald S Middleton, Laura Foster, Laura Barker, Piet Van Der Graaf, Peter Stacey, Christopher Kohl, Sara Coggon, Kevin Beaumont.   

Abstract

A series of substituted glutaramides were synthesised using Candoxatrilat 1 as a lead and evaluated for potency against neutral endopeptidase (NEP) as a potential treatment for female sexual arousal disorder (FSAD). In this paper, we describe studies in which we were able to increase NEP activity substantially over the levels reported for previous compounds from this programme by appropriate substitution in both the P(1)(') and P(2)(') regions. Optimisation led to the 4-chlorophenpropylamide S-30 which was selected as a candidate for further study.

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Year:  2006        PMID: 17070062     DOI: 10.1016/j.bmc.2006.10.002

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  4 in total

1.  Cyclopropyl-containing positive allosteric modulators of metabotropic glutamate receptor subtype 5.

Authors:  Sirish K Lakkaraju; Hannah Mbatia; Marie Hanscom; Zaorui Zhao; Junfang Wu; Bogdan Stoica; Alexander D MacKerell; Alan I Faden; Fengtian Xue
Journal:  Bioorg Med Chem Lett       Date:  2015-04-20       Impact factor: 2.823

Review 2.  It Is Not Taboo: Addressing Sexual Function in Adults with Congenital Heart Disease.

Authors:  Sihong Huang; Stephen C Cook
Journal:  Curr Cardiol Rep       Date:  2018-08-22       Impact factor: 2.931

3.  Cyclopropyl- and methyl-containing inhibitors of neuronal nitric oxide synthase.

Authors:  Huiying Li; Fengtian Xue; James M Kraus; Haitao Ji; Kristin Jansen Labby; Jan Mataka; Silvia L Delker; Pavel Martásek; Linda J Roman; Thomas L Poulos; Richard B Silverman
Journal:  Bioorg Med Chem       Date:  2012-12-22       Impact factor: 3.641

4.  Effects of Sacubitril/Valsartan on Physical and Social Activity Limitations in Patients With Heart Failure: A Secondary Analysis of the PARADIGM-HF Trial.

Authors:  Alvin Chandra; Eldrin F Lewis; Brian L Claggett; Akshay S Desai; Milton Packer; Michael R Zile; Karl Swedberg; Jean L Rouleau; Victor C Shi; Martin P Lefkowitz; Tzvetana Katova; John J V McMurray; Scott D Solomon
Journal:  JAMA Cardiol       Date:  2018-06-01       Impact factor: 14.676

  4 in total

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