2. Academic Validation
  3. Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder

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

  • Bioorg Med Chem. 2007 Jan 1;15(1):142-59. doi: 10.1016/j.bmc.2006.10.002.
David C Pryde 1,  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
Affiliations

Affiliation

  • 1 Department of Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. David.Pryde@Pfizer.com
PMID: 17070062 DOI: 10.1016/j.bmc.2006.10.002
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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