| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371812 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
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, IC50 = 43 nM) and impressive ability to penetrate brain in mice (brain/plasma ratio: 1.4).
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Zhicai Wu, 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,