Author/Authors :
David C. Pryde، نويسنده , , Andrew S. Cook، نويسنده , , Denise J. Burring، نويسنده , , Lyn H. Jones، نويسنده , , Stephanie Foll، نويسنده , , Michelle Y. Platts، نويسنده , , Vivienne Sanderson، نويسنده , , Martin Corless، نويسنده , , Alan Stobie، نويسنده , , Donald S. Middleton، نويسنده , , Laura Foster، نويسنده , , Laura Barker، نويسنده , , Piet Van Der Graaf، نويسنده , , Peter Stacey، نويسنده , , Christopher Kohl، نويسنده , , Sara Coggon، نويسنده , , Kevin Beaumont، نويسنده ,
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 image and image regions. Optimisation led to the 4-chlorophenpropylamide S-30 which was selected as a candidate for further study.
Keywords :
FSAD , Neutral endopeptidase , NEP , Glutaramides
