| Literature DB >> 22290078 |
Zhicai Wu1, Cangming Yang, Thomas H Graham, Andreas Verras, Renee M Chabin, Suoyu Xu, Xinchun Tong, Dan Xie, Mike E Lassman, Urmi R Bhatt, Margarita M Garcia-Calvo, Zhu Shen, Qing Chen, Kelly Bleasby, Ranabir Sinharoy, Jeffrey J Hale, James R Tata, Shirly Pinto, Steven L Colletti, Dong-Ming Shen.
Abstract
Efforts were dedicated to develop potent and brain penetrant prolylcarboxypeptidase (PrCP) inhibitors by replacing the amide group of original leads 1 and 2 with heterocycles. Aminopyrimidines including compound 32a were identified to display good PrCP inhibitory activity (32a, IC(50)=43 nM) and impressive ability to penetrate brain in mice (brain/plasma ratio: 1.4).Entities:
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Year: 2012 PMID： 22290078 DOI： 10.1016/j.bmcl.2011.12.098
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823