Synthesis and enzymatic evaluation of novel partially fluorinated thiol dual ACE/NEP inhibitors.
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Olimpieri F, Tambaro S, Fustero S, Lazzari P, Sanchez-Rosello M, Pani L, Volonterio A, Zanda M
Synthesis and enzymatic evaluation of novel partially fluorinated thiol dual ACE/NEP inhibitors.
Bioorg Med Chem Lett. 2009 Aug 15;19(16):4715-9. doi: 10.1016/j.bmcl.2009.06.064. Epub 2009 Jun 21.
- PubMed ID
- 19596577 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Captopril Angiotensin-converting enzyme IC 50 (nM) 0.12 N/A N/A Details