190269-86-4Relevant academic research and scientific papers
Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivatives
Meurer, Laura C.,Finke, Paul E.,Owens, Karen A.,Tsou, Nancy N.,Ball, Richard G.,Mills, Sander G.,MacCoss, Malcolm,Sadowski, Sharon,Cascieri, Margaret A.,Tsao, Kwei-Lan,Chicchi, Gary G.,Egger, Linda A.,Luell, Silvi,Metzger, Joseph M.,MacIntyre, D. Euan,Rupniak, Nadia M.J.,Williams, Angela R.,Hargreaves, Richard J.
, p. 4504 - 4511 (2006)
The synthesis and optimization of a cyclopentane-based hNK1 antagonist scaffold 3, having four chiral centers, will be discussed in the context of its enhanced water solubility properties relative to the marketed anti-emetic hNK1 antagonist EMEND (Aprepitant). Sub-nanomolar hNK1 binding was achieved and oral activity comparable to Aprepitant in two in vivo models will be described.
