Bioorganic and Medicinal Chemistry p. 142 - 159 (2007)
Update date:2022-08-02
Topics:
Pryde, David C.
Cook, Andrew S.
Burring, Denise J.
Jones, Lyn H.
Foll, Stephanie
Platts, Michelle Y.
Sanderson, Vivienne
Corless, Martin
Stobie, Alan
Middleton, Donald S.
Foster, Laura
Barker, Laura
Van Der Graaf, Piet
Stacey, Peter
Kohl, Christopher
Coggon, Sara
Beaumont, Kevin
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 P1′ and P2′ regions. Optimisation led to the 4-chlorophenpropylamide S-30 which was selected as a candidate for further study.
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