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Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder. Synthesis and activity of functionalized glutaramides

…, R Russell, L Foster, L Barker, C Wayman…

文献索引:Pryde, David C.; Maw, Graham N.; Planken, Simon; Platts, Michelle Y.; Sanderson, Vivienne; Corless, Martin; Stobie, Alan; Barber, Christopher G.; Russell, Rachel; Foster, Laura; Barker, Laura; Wayman, Christopher; Van Der Graaf, Piet; Stacey, Peter; Morren, Debbie; Kohl, Christopher; Beaumont, Kevin; Coggon, Sara; Tute, Michael Journal of Medicinal Chemistry, 2006 , vol. 49, # 14 p. 4409 - 4424

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被引用次数: 28

摘要

Female sexual arousal disorder (FSAD) is a highly prevalent sexual disorder affecting up to 40% of women. We describe herein our efforts to identify a selective neutral endopeptidase (NEP) inhibitor as a potential treatment for FSAD. The rationale for this approach, together with a description of the medicinal chemistry strategy, lead compounds, and SAR investigations are detailed. In particular, the strategy of starting with the clinically ...