| Literature DB >> 21515054 |
Melanie S Glossop1, Richard J Bazin, Kevin N Dack, David N A Fox, Graeme A MacDonald, Mark Mills, Dafydd R Owen, Chris Phillips, Keith A Reeves, Tracy J Ringer, Ross S Strang, Christine A L Watson.
Abstract
Heteroarylalanine derivatives 4 were designed as potential inhibitors of neutral endopeptidase (NEP EC 3.4.24.11). Selectivity over other zinc metalloproteinases was explored through occupation of the S2' subsite within NEP. Structural optimisation led to the identification of 5-phenyl oxazole 4f, a potent and selective NEP inhibitor. A crystal structure of the inhibitor bound complex is reported.Entities:
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Year: 2011 PMID： 21515054 DOI： 10.1016/j.bmcl.2011.03.109
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823