PMID

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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

 

Dual metalloprotease inhibitors. I. constrained peptidomimetics of mercaptoacyl dipeptides

TBA

Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.

Universite£

Novelß-amino acid derivatives as inhibitors of cathepsin A.

Sanofi-Aventis Deutschland

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)

Targeting ACE and ECE with dual acting inhibitors.

Universit£

Designed multiple ligands. An emerging drug discovery paradigm.

Organon Laboratories

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

Design and synthesis of potent, selective inhibitors of endothelin-converting enzyme.

Novartis Pharmaceuticals

Potent and systemically active aminopeptidase N inhibitors designed from active-site investigation.

University Of Paris

 

Potent non-peptidic dual inhibitors of endothelin-converting enzyme and neutral endopeptidase 24.11

TBA

 

Synthesis and evaluation of 2-(biphenylmethyl)glutaric acid amide derivatives as neutral endopeptidase inhibitors.

TBA

 

Solid phase synthesis of phosphinic acid endothelin converting enzyme inhibitors

TBA

 

Dual inhibition of neutral endopeptidase and angiotensin-converting enzyme by N-phosphonomethyl and N-carboxyalkyl dipeptides

TBA

Structure-based design of dipeptide derivatives for the human neutral endopeptidase.

Kao

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

 

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

 

Non-peptidic inhibitors of neutral endopeptidase 24.11 2. Design and pharmacology of orally active phosphonate prodrugs

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

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

Molecular Basis for Omapatrilat and Sampatrilat Binding to Neprilysin-Implications for Dual Inhibitor Design with Angiotensin-Converting Enzyme.

University Of Bath

Structure-Guided Design of Substituted Biphenyl Butanoic Acid Derivatives as Neprilysin Inhibitors.

Novartis Institutes For Biomedical Research

Meta-substituted benzofused macrocyclic lactams as zinc metalloprotease inhibitors.

Ciba-Geigy

Ortho-substituted benzofused macrocyclic lactams as zinc metalloprotease inhibitors.

Novartis Pharmaceuticals

Discovery of TD-0212, an Orally Active Dual Pharmacology AT

Theravance Biopharma Us

A mechanism-based inactivation study of neutral endopeptidase 24.11.

Salk Biotechnology/Industrial Associates

New dual inhibitors of neutral endopeptidase and angiotensin-converting enzyme: rational design, bioavailability, and pharmacological responses in experimental hypertension.

University Of Paris

Substituted?-mercaptoketones, new types of specific neprilysin inhibitors.

Pharmaleads

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

Discovery of nonsteroidal androgens.

University Of Tennessee At Memphis