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Bioorg Med Chem Lett. 2011 Jun 1;21(11):3404-6. doi: 10.1016/j.bmcl.2011.03.109. Epub 2011 Apr 5.

Synthesis and evaluation of heteroarylalanine diacids as potent and selective neutral endopeptidase inhibitors.

Author information

1
Pfizer Global Research and Development, Ramsgate Road, Sandwich CT13 9NJ, UK. mel.s.glossop@pfizer.com

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.

PMID:
21515054
DOI:
10.1016/j.bmcl.2011.03.109
[Indexed for MEDLINE]

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