118786-35-9Relevant academic research and scientific papers
Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder
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
, p. 142 - 159 (2007/10/03)
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.
GLUTARAMIDE DIURETIC AGENTS
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, (2008/06/13)
A series of novel spiro-substituted glutaramide derivatives have been prepared, including the pharmaceutically acceptable salts thereof and bioprecursors therefor, wherein the spiro-substituent completes a 5-or 6-membered carbocycyclic ring and is located at the carbon atom adjacent to the carbamoyl group. These particular compounds are inhibitors of the neutral endopeptidase E.C.3.4.24.11 enzyme and are therefore useful in therapy as diuretic agents for the treatment of hypertension, heart failure, renal insufficiency and other disorders. Methods for preparing these compounds from known starting materials are provided.
