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

Basic Information

ID: ALA1154033

Journal: Bioorg Med Chem Lett

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

Authors: Olimpieri F, Tambaro S, Fustero S, Lazzari P, Sanchez-Roselló M, Pani L, Volonterio A, Zanda M.

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.

CiteXplore: 19596577

DOI: 10.1016/j.bmcl.2009.06.064

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