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Bioorg Med Chem Lett. 2009 Aug 15;19(16):4715-9. doi: 10.1016/j.bmcl.2009.06.064. Epub 2009 Jun 21.

Synthesis and enzymatic evaluation of novel partially fluorinated thiol dual ACE/NEP inhibitors.

Author information

1
Dipartimento di Chimica, Materiali, e Ingegneria Chimica Giulio Natta, 20131 Milano, Italy.

Abstract

A novel family of peptidomimetics incorporating fluoroalkyl groups, mainly a trifluoromethyl, in alpha-position to a zinc(II)-binding thiol function, was synthesized in solution as well as in solid-phase. These compounds showed inhibitory potency in the nanomolar range against both angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP), whereas no inhibition of endothelin-converting enzyme-1 (ECE-1) was observed. The trifluoromethyl-derivatives were more potent than the parent unfluorinated analogues in the case of ACE, and less potent in the case of NEP.

PMID:
19596577
DOI:
10.1016/j.bmcl.2009.06.064
[Indexed for MEDLINE]

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