A novel family of peptidomimetics incorporating fluoroalkyl groups, mainly a trifluoromethyl, in α-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. © 2009 Elsevier Ltd. All rights reserved.
Synthesis and enzymatic evaluation of novel partially fluorinated thiol dual ACE/NEP inhibitors / Olimpieri, F.; Tambaro, S.; Fustero, S.; Lazzari, P.; Sanchez-Rosello, M.; Pani, L.; Volonterio, A.; Zanda, M.. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 19:16(2009), pp. 4715-4719. [10.1016/j.bmcl.2009.06.064]
Synthesis and enzymatic evaluation of novel partially fluorinated thiol dual ACE/NEP inhibitors
Lazzari P.;Pani L.;
2009
Abstract
A novel family of peptidomimetics incorporating fluoroalkyl groups, mainly a trifluoromethyl, in α-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. © 2009 Elsevier Ltd. All rights reserved.
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