111 articles for thisTarget
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Influence of polar side chains modifications on the dual enkephalinase inhibitory activity and conformation of human opiorphin, a pain perception related peptide.
Institute of Advanced Chemistry of Catalonia (Iqac-Csic)
Modulation of disulfide dual ENKephalinase inhibitors (DENKIs) activity by a transient N-protection for pain alleviation by oral route.
Pharmaleads
New orally active dual enkephalinase inhibitors (DENKIs) for central and peripheral pain treatment.
Pharmaleads
Discovery of the first potent and selective Mycobacterium tuberculosis Zmp1 inhibitor.
University of Siena
Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-ß hydrolysis.
University of Lille
Thiol-based angiotensin-converting enzyme 2 inhibitors: P1 modifications for the exploration of the S1 subsite.
Glaxosmithkline
Dual metalloprotease inhibitors. III. utilization of bicyclic and monocyclic diazepinone based mercaptoacetyls
TBA
Dual metalloprotease inhibitors. II. Effect of substitution and stereochemistry on benzazepinone based mercaptoacetyls
TBA
Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.
Universite£
Remarkable potential of thea-aminophosphonate/phosphinate structural motif in medicinal chemistry.
Wroclaw University of Technology
Proposed Bioactive Conformations of Opiorphin, an Endogenous Dual APN/NEP Inhibitor.
TBA
Structure-activity relationship study of opiorphin, a human dual ectopeptidase inhibitor with antinociceptive properties.
Institute of Advanced Chemistry of Catalonia (Iqac-Csic)
Synthesis and enzymatic evaluation of novel partially fluorinated thiol dual ACE/NEP inhibitors.
Dipartimento Di Chimica
Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells.
University Institute of Pathology
Computer-aided selection of potential antihypertensive compounds with dual mechanism of action.
Institute of Biomedical Chemistry of Russian Academy of Medical Sciences
Long lasting antinociceptive properties of enkephalin degrading enzyme (NEP and APN) inhibitor prodrugs.
University of Paris
Phosphinic derivatives as new dual enkephalin-degrading enzyme inhibitors: synthesis, biological properties, and antinociceptive activities.
University of Paris
Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action.
Novartis Institute For Biomedical Research
Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents.
F. Hoffmann-La Roche
Investigation of subsite preferences in aminopeptidase A (EC 3.4.11.7) led to the design of the first highly potent and selective inhibitors of this enzyme.
University of Paris
Design and synthesis of potent, selective inhibitors of endothelin-converting enzyme.
Novartis Pharmaceuticals
Optimal recognition of neutral endopeptidase and angiotensin-converting enzyme active sites by mercaptoacyldipeptides as a means to design potent dual inhibitors.
University of Paris
Design of orally active dual inhibitors of neutral endopeptidase and angiotensin-converting enzyme with long duration of action.
University of Paris
New alpha-thiol dipeptide dual inhibitors of angiotensin-I converting enzyme and neutral endopeptidase EC 3.4.24.11.
Ciba-Geigy
Hydroxamic acids as potent inhibitors of endothelin-converting enzyme from human bronchiolar smooth muscle.
Berlex Laboratories
N-Phosphonomethyl dipeptides and their phosphonate prodrugs, a new generation of neutral endopeptidase (NEP, EC 3.4.24.11) inhibitors.
Ciba-Geigy
New thiol inhibitors of neutral endopeptidase EC 3.4.24.11: synthesis and enzyme active-site recognition.
University of Paris
Design and synthesis of an orally active macrocyclic neutral endopeptidase 24.11 inhibitor.
Ciba-Geigy
Potent and systemically active aminopeptidase N inhibitors designed from active-site investigation.
University of Paris
Retro-inverso concept applied to the complete inhibitors of enkephalin-degrading enzymes.
Ua 498 Cnrs
Synthesis and biological evaluation of phosphonamidate peptide inhibitors of enkephalinase and angiotensin-converting enzyme.
TBA
New bidentates as full inhibitors of enkephalin-degrading enzymes: synthesis and analgesic properties.
TBA
New carboxyalkyl inhibitors of brain enkephalinase: synthesis, biological activity, and analgesic properties.
TBA
Potent non-peptidic dual inhibitors of endothelin-converting enzyme and neutral endopeptidase 24.11
TBA
Design and synthesis of phosphinic acids that triply inhibit endothelin converting enzyme, angiotensin converting enzyme and neutral endopeptidase 24.11
TBA
Synthesis and evaluation of 2-(biphenylmethyl)glutaric acid amide derivatives as neutral endopeptidase inhibitors.
TBA
Potent inhibitors of neutral endopeptidase. 2-Biphenyl- methylglutaric acid amide derivatives
TBA
Dual inhibition of neutral endopeptidase and angiotensin-converting enzyme by N-phosphonomethyl and N-carboxyalkyl dipeptides
TBA
4-Substituted proline derivatives that inhibit angiotensin converting enzyme and neutral endopeptidase 24.11.
TBA
Mercaptoacyl dipeptides as dual inhibitors of angiotensin-converting enzyme and neutral endopeptidase. Preliminary structure-activity studies
TBA
Aminophosphonate endothelin converting enzyme inhibitors: potency-enhancing and selectivity-improving modifications of phosphoramidon
TBA
Synthesis and evaluation of heteroarylalanine diacids as potent and selective neutral endopeptidase inhibitors.
Pfizer
Phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1 inhibitors.
Cea
The synthesis of aminobenzazepinones as anti-phenylalanine dipeptide mimics and their use in nep inhibition
TBA
Dual inhibition of angiotensin-converting enzyme and neutral endopeptidase by tricyclic benzazepinone thiols
TBA
Studies on the structural feature of S'1 subsite of neprilysin (EC.3.4.24.11): Stereochemical requirement for the enzyme-inhibitor docking process
TBA
Design and synthesis of a new class of conformationally constrained inhibitors to probe the active sites of thermolysine and neutral endopeptidase 24.11
TBA
α-Mercaptoacyl dipeptides that inhibit angiotensin converting enzyme and neutral endopeptidase 24.11
TBA
Non-peptidic inhibitors of neutral endopeptidase 24.11 2. Design and pharmacology of orally active phosphonate prodrugs
TBA
Non-peptidic inhibitors of neutral endopeptidase 24.11 1. Discovery and optimization of potency
TBA
The effect of heteroatom substitution on a series of phosphonate inhibitors of neutral endopeptidase 24.11
TBA
Gem-cycloalkyl substituted thiol inhibitors of neutral endopeptidase 24.11. Synthesis via nucleophilic opening of 2,2-spiro-β-lactones
TBA
Synthesis of 6-amino-5-oxo-7-phenyl-1,4-oxazepines as conformationally constrained gauche (−) dipeptide mimetics
TBA
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
University of Athens
Homology modeling and site-directed mutagenesis to identify selective inhibitors of endothelin-converting enzyme-2.
Mount Sinai School of Medicine
Thiol-based angiotensin-converting enzyme 2 inhibitors: P1' modifications for the exploration of the S1' subsite.
Glaxosmithkline
Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder.
Pfizer
Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder. Synthesis and activity of functionalized glutaramides.
Pfizer
Probing the Requirements for Dual Angiotensin-Converting Enzyme C-Domain Selective/Neprilysin Inhibition.
University of Cape Town
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
University of Nebraska Medical Center
N-[2-(Indan-1-yl)-3-mercapto-propionyl] amino acids as highly potent inhibitors of the three vasopeptidases (NEP, ACE, ECE): In vitro and In vivo activities.
University of Paris
Asymmetric synthesis of BB-3497--a potent peptide deformylase inhibitor.
British Biotech Pharmaceuticals
2-(2-Oxo-1,4-dihydro-2H-quinazolin-3-yl)- and 2-(2,2-dioxo-1,4-dihydro-2H-2lambda6-benzo[1,2,6]thiadiazin-3-yl)-N-hydroxy-acetamides as potent and selective peptide deformylase inhibitors.
F. Hoffmann-La Roche
N-formyl hydroxylamine containing dipeptides: generation of a new class of vasopeptidase inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Molecular Basis for Omapatrilat and Sampatrilat Binding to Neprilysin-Implications for Dual Inhibitor Design with Angiotensin-Converting Enzyme.
University of Bath
Vasopeptidase inhibitors: incorporation of geminal and spirocyclic substituted azepinones in mercaptoacyl dipeptides.
The Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-Guided Design of Substituted Biphenyl Butanoic Acid Derivatives as Neprilysin Inhibitors.
Novartis Institutes For Biomedical Research
Highly selective and orally active inhibitors of type IV collagenase (MMP-9 and MMP-2): N-sulfonylamino acid derivatives.
Shionogi
Meta-substituted benzofused macrocyclic lactams as zinc metalloprotease inhibitors.
Ciba-Geigy
Ortho-substituted benzofused macrocyclic lactams as zinc metalloprotease inhibitors.
Novartis Pharmaceuticals
Dual metalloprotease inhibitors. 6. Incorporation of bicyclic and substituted monocyclic azepinones as dipeptide surrogates in angiotensin-converting enzyme/neutral endopeptidase inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and analgesic effects of N-[3-[(hydroxyamino) carbonyl]-1-oxo-2(R)-benzylpropyl]-L-isoleucyl-L-leucine, a new potent inhibitor of multiple neurotensin/neuromedin N degrading enzymes.
Ccipe-Faculté
Exploration of neutral endopeptidase active site by a series of new thiol-containing inhibitors.
University of Paris
Application of a conformationally restricted Phe-Leu dipeptide mimetic to the design of a combined inhibitor of angiotensin I-converting enzyme and neutral endopeptidase 24.11.
Marion Merrell Dow Research Institute
A mechanism-based inactivation study of neutral endopeptidase 24.11.
Salk Biotechnology/Industrial Associates
Heterocyclic lactam derivatives as dual angiotensin converting enzyme and neutral endopeptidase 24.11 inhibitors.
Ciba-Geigy
New dual inhibitors of neutral endopeptidase and angiotensin-converting enzyme: rational design, bioavailability, and pharmacological responses in experimental hypertension.
University of Paris
Mercaptoacyl amino acid inhibitors of atriopeptidase. 1. Structure-activity relationship studies of methionine and S-alkylcysteine derivatives.
Schering-Plough Research Institute
1H NMR configurational correlation for retro-inverso dipeptides: application to the determination of the absolute configuration of"enkephalinase" inhibitors. Relationships between stereochemistry and enzyme recognition.
TBA
New kelatorphan-related inhibitors of enkephalin metabolism: improved antinociceptive properties.
University of Paris
Carboxyalkyl dipeptides with atrial natriuretic factor potentiating and antihypertensive activity.
Schering-Plough Research Institute
A novel class of enkephalinase inhibitors containing a C-terminal sulfo group.
Dainippon Pharmaceutical
Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.
Ranbaxy Laboratories
In vitro inhibition effect and structure-activity relationships of some saccharin derivatives on erythrocyte carbonic anhydrase I and II.
Sakarya University
Inhibitors of human mitotic kinesin Eg5: characterization of the 4-phenyl-tetrahydroisoquinoline lead series.
Bristol-Myers Squibb
The First Biologically Active Synthetic Analogues of FK228, the Depsipeptide Histone Deacetylase Inhibitor.
University of Southampton