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Differential Structure‐Activity Relationships of Phosphoramidon Analogues for Inhibition of Three Metalloproteases: Endothelin‐Converting Enzyme, Neutral Endopeptidase, and Angiotensin‐Converting
TLDR
It is suggested that a hydrophobic group in the P1 position of phosphoramidon analogues increases the potency for ECE significantly, whereas compounds containing a free phosphonic acid are optimal for inhibition of NEP and ACE.
Dicarboxylic acid dipeptide neutral endopeptidase inhibitors.
The synthesis of three series of dicarboxylic acid dipeptide neutral endopeptidase 24.11 (NEP) inhibitors is described. In particular, the amino butyramide 21a exhibited potent NEP inhibitory
Pharmacological profile of a non-peptidic dual inhibitor of neutral endopeptidase 24.11 and endothelin-converting enzyme.
TLDR
Results suggest that CGS 26303 represents a new class of therapeutic agents with potential benefits for the treatment of cardiovascular and renal disorders.
New alpha-thiol dipeptide dual inhibitors of angiotensin-I converting enzyme and neutral endopeptidase EC 3.4.24.11.
TLDR
A novel series of alpha-thio dipeptides containing central cyclic non-natural amino acids were prepared and were evaluated for their ability to inhibit these two metallopeptidases in vitro and in vivo and several were found to be excellent dual inhibitors of ACE and NEP in vitro.
Disposition of thiorphan in DOCA-salt and spontaneously hypertensive rats.
TLDR
Results indicate that reduced clearance of thiorphan in DOCA-salt rats may be due to the co-administration of DOCA -salt or altered renal function of the hypertrophic remaining kidney and not solely due to hypertension.
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