Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder.
Pryde DC,
Cook AS,
Burring DJ,
Jones LH,
Foll S,
Platts MY,
Sanderson V,
Corless M,
Stobie A,
Middleton DS,
Foster L,
Barker L,
Van Der Graaf P,
Stacey P,
Kohl C,
Coggon S,
Beaumont K.
Department of Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. David.Pryde@Pfizer.com
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.
PMID: 17070062 [PubMed - indexed for MEDLINE]