1350711-76-0Relevant articles and documents
Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors
Debenham, John S.,Graham, Thomas H.,Verras, Andreas,Zhang, Yong,Clements, Matthew J.,Kuethe, Jeffrey T.,Madsen-Duggan, Christina,Liu, Wensheng,Bhatt, Urmi R.,Chen, Dunlu,Chen, Qing,Garcia-Calvo, Margarita,Geissler, Wayne M.,He, Huaibing,Li, Xiaohua,Lisnock, Jeanmarie,Shen, Zhu,Tong, Xinchun,Tung, Elaine C.,Wiltsie, Judyann,Xu, Suoyu,Hale, Jeffrey J.,Pinto, Shirly,Shen, Dong-Ming
, p. 6228 - 6233 (2013/11/19)
The synthesis, SAR, binding affinities and pharmacokinetic profiles are described for a series of cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors discovered by high throughput screening. Compounds show high levels of ex vivo target engagement in mouse plasma 20 h post oral dose.