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Discovery of a new class of potent prolylcarboxypeptidase inhibitors derived from alanine |
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| Authors: | Wu Zhicai Yang Cangming Xiong Yusheng Feng Zhe Lombardo Matthew Verras Andreas Chabin Renee M Xu Suoyu Tong Xinchun Xie Dan Lassman Mike E Bhatt Urmi R Garcia-Calvo Margarita M Geissler Wayne Shen Zhu Chen Qing Sinharoy Ranabir Hale Jeffrey J Tata James R Pinto Shirly Shen Dong-Ming Colletti Steven L |
| Affiliation: | Department of Discovery Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. zhicai_wu@merck.com |
| Abstract: | Efforts to modify the central proline portion of lead compound 4 lead to the discovery of novel prolylcarboxypeptidase (PrCP) inhibitors. Especially, replacement with alanine afforded compound 19 displaying more potent human and mouse PrCP inhibitory activity than 4 and an overall comparable profile. |
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