PMID

Data

Article Title

Organization

Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.

Novartis Pharma

Structure-Based Library Design and Fragment Screening for the Identification of Reversible Complement Factor D Protease Inhibitors.

Novartis Institutes For Biomedical Research

Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing.

Bristol-Myers Squibb Research and Development

Evaluation of bisbenzamidines as inhibitors for matriptase-2.

University of Bonn

Neutrophil elastase inhibitors for the treatment of (cardio)pulmonary diseases: Into clinical testing with pre-adaptive pharmacophores.

Bayer Healthcare

Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors.

Southeast University

Discovery of a Cyclic Boronic Acidß-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.

Rempex Pharmaceuticals

Synthesis and pharmacological characterization of 2-aminobenzaldehyde oxime analogs as dual inhibitors of neutrophil elastase and proteinase 3.

Chang Gung University

Neutrophil elastase inhibitors as potential anti-inflammatory therapies.

Therachem Research Medilab (India)

How aß-D-glucoside side chain enhances binding affinity to thrombin of inhibitors bearing 2-chlorothiophene as P1 moiety: crystallography, fragment deconstruction study, and evaluation of antithrombotic properties.

Consiglio Nazionale Delle Ricerche

Proteinase inhibitors. I. Inhibitors of elastase.

TBA

Novel bis(benzamidino) compounds with an aromatic central link. Inhibitors of thrombin, pancreatic kallikrein, trypsin, and complement.

TBA

Diarylamidine derivatives with one or both of the aryl moieties consisting of an indole or indole-like ring. Inhibitors of arginine-specific esteroproteases.

TBA

Inactivation of trypsin-like proteases by sulfonylation. Variation of positively charged group and inhibitor length.

TBA

Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase.

Universidad De Buenos Aires

Optimization of O3-acyl kojic acid derivatives as potent and selective human neutrophil elastase inhibitors.

Universidade De Lisboa

Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.

Emory University

Synthesis and biological evaluation of direct thrombin inhibitors bearing 4-(piperidin-1-yl)pyridine at the P1 position with potent anticoagulant activity.

University of Bari &Quot;Aldo Moro&Quot

Optimization of N-benzoylindazole derivatives as inhibitors of human neutrophil elastase.

Universit£

Discovery of novel series of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as human chymase inhibitors using structure-based drug design.

Asubio Pharma

Potent elastase inhibitors from cyanobacteria: structural basis and mechanisms mediating cytoprotective and anti-inflammatory effects in bronchial epithelial cells.

University of Florida

Design and synthesis of 4H-3,1-benzoxazin-4-ones as potent alternate substrate inhibitors of human leukocyte elastase.

Syntex Research

Inhibition of human leukocyte elastase, porcine pancreatic elastase, and chymotrypsin by elasnin and other 4-hydroxy-2-pyrones.

TBA

Thrombin inhibitors. 2. Amide derivatives of N alpha-substituted L-arginine.

TBA

Thrombin inhibitors. 1. Ester derivatives of N alpha-(arylsulfonyl)-L-arginine.

TBA

Synopsis of some recent tactical application of bioisosteres in drug design.

Bristol-Myers Squibb Pharmaceutical Research and Development

Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.

Aarhus University

Thrombin inhibitors from the freshwater cyanobacterium Anabaena compacta.

Hokkaido University

N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases.

University of Lisbon

Development of tryptase inhibitors derived from thalidomide.

The University of Tokyo

Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.

Merck Research Laboratories

X-ray snapshot of the mechanism of inactivation of human neutrophil elastase by 1,2,5-thiadiazolidin-3-one 1,1-dioxide derivatives.

Wichita State University

Bornyl (3,4,5-trihydroxy)-cinnamate--an optimized human neutrophil elastase inhibitor designed by free energy calculations.

Albert-Ludwigs-University of Freiburg

Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.

Johnson & Johnson Pharmaceutical Research & Development

Azetidine-2,4-diones (4-oxo-beta-lactams) as scaffolds for designing elastase inhibitors.

Universidade De Lisboa

Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.

Cephalon

Resisting degradation by human elastase: commonality of design features shared by 'canonical' plant and bacterial macrocyclic protease inhibitor scaffolds.

Imperial College

Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties.

University of Antwerp

Design and synthesis of depeptidized macrocyclic inhibitors of hepatitis C NS3-4A protease using structure-based drug design.

Schering-Plough Research Institute

Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151).

Gsk

Simple, intuitive calculations of free energy of binding for protein-ligand complexes. 1. Models without explicit constrained water.

University of Parma

Development of orally active nonpeptidic inhibitors of human neutrophil elastase.

Cortech

Estimation of binding affinities for selective thrombin inhibitors via Monte Carlo simulations.

Yale University

Protease inhibitors: current status and future prospects.

University of Queensland

GRID/CPCA: a new computational tool to design selective ligands.

Boehringer Ingelheim Pharma

Design and synthesis of thrombin inhibitors: analogues of MD-805 with reduced stereogenicity and improved potency.

Novartis Horsham Research Centre

Synthesis and structure-activity relationships of potent thrombin inhibitors: piperazides of 3-amidinophenylalanine.

Klinikum Der Friedrich-Schiller-Universit£T Jena

Discovery and biological activity of orally active peptidyl trifluoromethyl ketone inhibitors of human neutrophil elastase.

Zeneca Pharmaceuticals

Inhibition of human neutrophil elastase with peptidyl electrophilic ketones. 2. Orally active PG-Val-Pro-Val pentafluoroethyl ketones.

Marion Merrell Dow Research Institute

2,6-Disubstituted aryl carboxylic acids, leaving groups"par excellence" for benzisothiazolone inhibitors of human leukocyte elastase.

Sterling Winthrop Pharmaceutical Research Division

Inhibition studies of some serine and thiol proteinases by new leupeptin analogues.

University of Arkansas

Novel anthraquinone inhibitors of human leukocyte elastase and cathepsin G.

Georgia Institute of Technology

Inhibition of human leukocyte elastase (HLE) by N-substituted peptidyl trifluoromethyl ketones.

Boehringer Ingelheim Pharmaceuticals

Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.

Merck Research Laboratories

Anticoagulant peptides: nature of the interaction of the C-terminal region of hirudin with a noncatalytic binding site on thrombin.

TBA

The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate.

Glaxowellcome Medicines Research Centre

Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine-trans-lactams.

Glaxowellcome Medicines Research Centre

Highly potent and selective peptide-based inhibitors of the hepatitis C virus serine protease: towards smaller inhibitors.

Boehringer Ingelheim Pharmaceuticals

Metallopeptide approach to the design of biologically active ligands: design of specific human neutrophil elastase inhibitors.

Palatin Technologies

HLE-inhibitory alkaloids with a polyketide skeleton from the marine-derived fungus Coniothyrium cereale.

University of Bonn

Design, synthesis and evaluation of N-benzoylindazole derivatives and analogues as inhibitors of human neutrophil elastase.

Universit£

Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.

Boehringer Ingelheim (Canada)

2-Azetidinone--a new profile of various pharmacological activities.

Barkatullah University

Inhibitors of human neutrophil elastase based on a highly functionalized N-amino-4-imidazolidinone scaffold.

Wichita State University

MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.

Merck Research Laboratories

Synthesis and evaluation of benzoxazinone derivatives on activity of human neutrophil elastase and on hemorrhagic shock-induced lung injury in rats.

Chang Gung University

Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.

Johnson & Johnson Pharmaceutical Research and Development

Potent inhibitors of beta-tryptase and human leukocyte elastase based on the MCoTI-II scaffold.

Imperial College

Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C.

Merck Frosst Canada

Evaluation of human neutrophil elastase inhibitory effect of iridoid glycosides from Hedyotis diffusa.

Korea Research Institute of Bioscience and Biotechnology

Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.

National Human Genome Research Institute

4-Oxo-beta-lactams (azetidine-2,4-diones) are potent and selective inhibitors of human leukocyte elastase.

University of Lisbon

Synthesis and optimization of 2-pyridin-3-yl-benzo[d][1,3]oxazin-4-one based inhibitors of human neutrophil elastase.

Activx Biosciences

Fluorinated benzyloxyphenyl piperidine-4-carboxamides with dual function against thrombosis: inhibitors of factor Xa and platelet aggregation.

University of Bari

Design of alternate substrate inhibitors of serine proteases. Synergistic use of alkyl substitution to impede enzyme-catalyzed deacylation.

TBA

 

Rational design of selective thrombin inhibitors

TBA

 

Inhibition of human cytomegalovirus protease by benzoxazinones and evidence of antiviral activity in cell culture

TBA

 

Synthesis of 7α-methoxy-2-(1,3-dithiolan-2-ylidene)cephem sulphones. A new series of human leukocyte elastase inhibitors

TBA

 

A comparative SAR and computer modeling study of benzisothiazolone, mechanism-based inhibitors with porcine pancreatic and human leukocyte elastase

TBA

 

(N-acyl-N-alkyl)glycyl borolysine analogs: A new class of potent thrombin inhibitors

TBA

 

Tricyclic cephems as inhibitors of human leukocyte elastase. thieno[3,4-c]cepham sulfones and pyrrolo[3,4-c]cepham sulfones

TBA

 

Tricyclic cephems as inhibitors of human leukocyte elastase. Furo[3,4-c]cepham sulfones

TBA

 

The design of potent and stable benzisothiazolone inhibitors of human leukocyte elastase

TBA

 

Inhibitors of human leukocyte elastase. 3.¹ inhibition by tetrahydrobenzisothiazolinylmethyl aryl carboxylates

TBA

 

Inhibitors of human leukocyte elastase. 2.¹ synthesis and sar of benzisothiazolinylmethyl aryl ethers

TBA

 

Phosphorous acid analogs of L-680,833, a potent monocyclic β-lactam inhibitor of human leukocyte elastase

TBA

 

Alkoxy substituted benzisothiazolone (BIT) derivatives: potent inhibitors of human leukocyte elastase

TBA

 

Synthesis and porcine pancreatic elastase inhibitory evaluation of 6α-(sulfonyl)oxy-and 6α-chloropenicillanate sulfone esters and 3α-(acyloxy)methyl-6α-chloropenam sulfones

TBA

 

1,3-Oxazino[4,5-b]indole-2,4-(1H,9H)-diones and 5,6-dimethylpyrrolo-[2,3-d]-1,3-oxazin-2,4-(1H,7H)-diones as serine protease inhi...

TBA

 

Synthesis of new thiazinoindole derivatives and their evaluation as inhibitors of human leukocyte elastase and other related serine proteases

TBA

 

Examination of peptidic α′,β-diamino-α,α-difluoroketones as inhibitors of human leukocyte elastase

TBA

 

A benzisothiazolone class of potent, selective mechanism-based inhibitors of human leukocyte elastase

TBA

 

elastase inhibitors containing conformationally restricted lactams as P₃-P₂ dipeptide replacements

TBA

 

Janus compounds: dual inhibitors of proteinases

TBA

 

Enantioselective synthesis and antielastase activity of 1,3,4-trisubstituted and 3,4-disubstituted β-lactam antibiotics

TBA

 

Inhibition of human leukocyte elastase. 7. Inhibition by 6-substituted penicillin amides.

TBA

 

Inhibition of human leukocyte elastase. 6. Inhibition by 6-substituted penicillin esters.

TBA

 

Inhibition of human leukocyte elastase. 5. Inhibition by 6-alkyl substituted penem benzyl esters.

TBA

 

Inhibition of human leukocyte elastase (HLE) by novel bicyclic β-lactams

TBA

 

Cephem sulfones as inactivators of human leukocyte elastase. II. Keto-enol tautomerish in cephem-4-ketones.

TBA

 

Characterization of LY806303 as a potent and selective inhibitor of thrombin

TBA

 

The effect of N-acyl substituents on the stability of monocyclic β-lactam inhibitors of human leukocyte elastase

TBA

 

Potential mechanism-based inhibitors of proteolytic enzymes

TBA

 

Synthesis of a peptidyl 2,2-difluoro-3-aminopropionate

TBA

 

A general synthesis of 4-alkyl/aryl substituted saccharins

TBA

Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2H)-one 1,1-dioxides.

University of Leipzig

Effects of tannins from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade.

National University of Singapore

Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors.

Daiichi Asubio Pharma

Cathepsin A is the major hydrolase catalyzing the intracellular hydrolysis of the antiretroviral nucleotide phosphonoamidate prodrugs GS-7340 and GS-9131.

Gilead Sciences

Ahp-Cyclodepsipeptides as tunable inhibitors of human neutrophil elastase and kallikrein 7: Total synthesis of tutuilamide A, serine protease selectivity profile and comparison with lyngbyastatin 7.

University of Florida

Covalent Small Molecule Immunomodulators Targeting the Protease Active Site.

National Cancer Institute

Design and discovery of boronic acid drugs.

Mcgill University

Recent developments of small molecules with anti-inflammatory activities for the treatment of acute lung injury.

Zhejiang University

Advances in research of spirodienone and its derivatives: Biological activities and synthesis methods.

Sichuan University

Design, synthesis and biological evaluation of P2-modified proline analogues targeting the HtrA serine protease in Chlamydia.

University of Otago

Why All the Fury over Furin?

University of Michigan

Pyridones in drug discovery: Recent advances.

Astrazeneca

Improving the selectivity of 3-amidinophenylalanine-derived matriptase inhibitors.

Philipps University

Boron-Containing heterocycles as promising pharmacological agents.

Long Island University

A systematic approach to the optimization of substrate-based inhibitors of the hepatitis C virus NS3 protease: discovery of potent and specific tripeptide inhibitors.

Boehringer Ingelheim (Canada)

1,5,6,7-Tetrahydro-4H-indazol-4-ones as human neutrophil elastase (HNE) inhibitors.

University of Florence

Elastase Inhibitor Cyclotheonellazole A: Total Synthesis and In Vivo Biological Evaluation for Acute Lung Injury.

Nankai University

Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy.

Bristol Myers Squibb

Optimization of peptide-based inhibitors targeting the HtrA serine protease in Chlamydia: Design, synthesis and biological evaluation of pyridone-based and N-Capping group-modified analogues.

University of Otago

Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.

3-Dimensional Pharmaceuticals

Synthesis and evaluation of delta-lactams (piperazones) as elastase inhibitors.

The Oxford Centre For Molecular Sciences and The Dyson Perrins Laboratory

Phenethyl amides as novel noncovalent inhibitors of hepatitis C virus NS3/4A protease: discovery, initial SAR, and molecular modeling.

Mrl Rome

3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors.

Currently Naeja Pharmaceutical

P1 Phenethyl peptide boronic acid inhibitors of HCV NS3 protease.

Bristol-Myers Squibb Pharmaceutical Research Institute

Clarification of mechanism of human sputum elastase inhibition by a new inhibitor, ONO-5046, using electrospray ionization mass spectrometry.

Minase Research Institute

Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry.

Endotherm

Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19.

Pfizer

The Basicity Makes the Difference: Improved Canavanine-Derived Inhibitors of the Proprotein Convertase Furin.

Philipps University

Design and synthesis of peptide-based carboxylic acid-containing transition-state inhibitors of human neutrophil elastase.

Dainippon Pharmaceutical

Exploration of nitrogen heterocycle scaffolds for the development of potent human neutrophil elastase inhibitors.

University of Florence

Novel bicyclic lactam inhibitors of thrombin: potency and selectivity optimization through P1 residues.

Shire Biochem

Design, Synthesis, and Pharmacological Characterization of a Neutral, Non-Prodrug Thrombin Inhibitor with Good Oral Pharmacokinetics.

Bayer

Lung Protection by Cathepsin C Inhibition: A New Hope for COVID-19 and ARDS?

Centre D'Etude Des Pathologies Respiratoires and Universit£

Synthesis and evaluation of the sunflower derived trypsin inhibitor as a potent inhibitor of the type II transmembrane serine protease, matriptase.

National Cancer Institute-Frederick

Facile Synthesis of Aminomethyl Phosphinate Esters as Serine Protease Inhibitors with Primed Site Interaction.

Ku Leuven

Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.

Shionogi

Design, synthesis and stability of N-acyloxymethyl- and N-aminocarbonyloxymethyl-2-azetidinones as human leukocyte elastase inhibitors.

Ineti

Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-?-lactamases.

Qpex Biopharma

The identification of alpha-ketoamides as potent inhibitors of hepatitis C virus NS3-4A proteinase.

Roche Discover Welwyn

Design and synthesis of new orally active nonpeptidic inhibitors of human neutrophil elastase.

Colorado State University

1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.

Shionogi

Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.

Shionogi

Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.

Roche Pharma Research and Early Development

Mass spectrometry reveals elastase inhibitors from the reactive centre loop of alpha1-antitrypsin.

The Oxford Centre For Molecular Sciences

Trypsin inhibitors for the treatment of pancreatitis.

Novartis Pharma

Optimization of Cyclic Plasmin Inhibitors: From Benzamidines to Benzylamines.

Philipps University Marburg

Suppression of Tumor Growth and Metastases by Targeted Intervention in Urokinase Activity with Cyclic Peptides.

Chinese Academy of Sciences

2-(diethylamino)thieno1,3??xazin-4-ones as stable inhibitors of human leukocyte elastase.

University of Leipzig

Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs).

School of Pharmaceutical Sciences & The Fifth Affiliated Hospital

2-chloro-3-substituted-1,4-naphthoquinone inactivators of human cytomegalovirus protease.

Glaxowellcome Medicines Research Centre

Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors.

Glaxosmithkline

Molecular structure of FR901277, a novel inhibitor of human leukocyte elastase, and its binding mode simulation.

Fujisawa Pharmaceutical

Applications of amide isosteres in medicinal chemistry.

Xenon Pharmaceuticals

Structure-activity analysis of peptidic Chlamydia HtrA inhibitors.

University of Otago

Structure guided drug design to develop kallikrein 5 inhibitors to treat Netherton syndrome.

Glaxosmithkline R&D

Synthesis and in vitro and in vivo evaluation of the 2-(6'methoxy-3',4'-dihydro-1'-naphtyl)-4H-3,1-benzoxazin-4- one as a new potent substrate inhibitor of human leukocyte elastase.

Università

Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.

Universit£T Bonn

Binding Loop Substitutions in the Cyclic Peptide SFTI-1 Generate Potent and Selective Chymase Inhibitors.

The University of Queensland

Structural and functional analyses of benzamidine-based inhibitors in complex with trypsin: implications for the inhibition of factor Xa, tPA, and urokinase.

Institut FüR Biochemie

5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.

Glaxo Wellcome Research and Development

Studies on the C-terminal of hexapeptide inhibitors of the hepatitis C virus serine protease.

Boehringer Ingelheim (Canada)

Boron in drug design: Recent advances in the development of new therapeutic agents.

S£O Paulo State University

Inhibition of human cytomegalovirus protease N(o) with monocyclic beta-lactams.

Boehringer Ingelheim (Canada)

Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.

Proscript

Preparation of alpha-keto ester enol acetates as potential prodrugs of human neutrophil elastase inhibitors.

Cinc

Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.

Biotech Research Institute

1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase.

Bristol-Myers Squibb Pharmaceutical Research Institute

Design and synthesis of hydrazinopeptides and their evaluation as human leukocyte elastase inhibitors.

Institut Jacques Monod (Umr Cnrs 7592/UniversitéS Paris Vi and Vii)

Design of benzamidine-type inhibitors of factor Xa.

Institut FüR Biochemie

Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition.

Glaxowellcome Medicines Research Centre

Ahp-Cyclodepsipeptide Inhibitors of Elastase: Lyngbyastatin 7 Stability, Scalable Synthesis, and Focused Library Analysis.

University of Florida

beta-Lactam derivatives as inhibitors of human cytomegalovirus protease.

Boehringer Ingelheim (Canada)

Inhibition of human neutrophil elastase. 4. Design, synthesis, X-ray crystallographic analysis, and structure-activity relationships for a series of P2-modified, orally active peptidyl pentafluoroethyl ketones.

Hoechst Marion Roussel

Novel thieno[2,3-d][1,3]oxazin-4-ones as inhibitors of human leukocyte elastase.

University of Leipzig

Peptidomimetic inhibitors of the human cytomegalovirus protease.

Boehringer Ingelheim

Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase.

Zeneca Pharmaceuticals

7-alkylidenecephalosporin esters as inhibitors of human leukocyte elastase.

Southern Methodist University

Anionic- and lipophilic-mediated surface binding inhibitors of human leukocyte elastase.

RhôNe-Poulenc Rorer

Dual inhibition of human leukocyte elastase and lipid peroxidation: in vitro and in vivo activities of azabicyclo[2.2.2]octane and perhydroindole derivatives.

Institut De Recherche Servier

Synthesis, anticancer activity, and molecular modeling of 1,4-naphthoquinones that inhibit MKK7 and Cdc25.

Montana State University

Iterative Optimization of the Cyclic Peptide SFTI-1 Yields Potent Inhibitors of Neutrophil Proteinase 3.

The University of Queensland

Nonpeptidic inhibitors of human neutrophil elastase. 7. Design, synthesis, and in vitro activity of a series of pyridopyrimidine trifluoromethyl ketones.

Zeneca Pharmaceuticals

Design of Specific Serine Protease Inhibitors Based on a Versatile Peptide Scaffold: Conversion of a Urokinase Inhibitor to a Plasma Kallikrein Inhibitor.

Aarhus University

Design of orally active, non-peptidic inhibitors of human leukocyte elastase.

Zeneca Pharmaceuticals Group

Cephem sulfones as inactivators of human leukocyte elastase. 5. 7 alpha-Methoxy- and 7 alpha-chloro-1,1-dioxocephem 4-ketones.

Pharmacia-Farmitalia Carlo Erba

Nonpeptidic inhibitors of human leukocyte elastase. 3. Design, synthesis, X-ray crystallographic analysis, and structure-activity relationships for a series of orally active 3-amino-6-phenylpyridin-2-one trifluoromethyl ketones.

Zeneca Pharmaceuticals Group

Nonpeptidic inhibitors of human leukocyte elastase. 2. Design, synthesis, and in vitro activity of a series of 3-amino-6-arylopyridin-2-one trifluoromethyl ketones.

Zeneca Pharmaceuticals Group

Non-peptidic inhibitors of human leukocyte elastase. 1. The design and synthesis of pyridone-containing inhibitors.

Zeneca

Orally bioavailable benzisothiazolone inhibitors of human leukocyte elastase.

Sterling Winthrop

Nonpeptidic inhibitors of human leukocyte elastase. 5. Design, synthesis, and X-ray crystallography of a series of orally active 5-aminopyrimidin-6-one-containing trifluoromethyl ketones.

Zeneca Pharmaceuticals

Non-peptidic inhibitors of human leukocyte elastase. 4. Design, synthesis, and in vitro and in vivo activity of a series of beta-carbolinone-containing trifluoromethyl ketones.

Zeneca Pharmaceuticals

Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 2. Effect of varying the heterocyclic ring on in vitro potency.

Zeneca Pharmaceuticals

Nonpeptidic inhibitors of human leukocyte elastase. 6. Design of a potent, intratracheally active, pyridone-based trifluoromethyl ketone.

Zeneca Pharmaceuticals

Inhibition of human neutrophil elastase. 3. An orally active enol acetate prodrug.

Marion Merrell Dow Research Institute

Phosphonates and phosphinates: novel leaving groups for benzisothiazolone inhibitors of human leukocyte elastase.

Sterling Winthrop Pharmaceuticals Research Division

New orally active serine protease inhibitors.

Minase Research Institute

Orally active beta-lactam inhibitors of human leukocyte elastase. 3. Stereospecific synthesis and structure-activity relationships for 3,3-dialkylazetidin-2-ones.

Merck Research Laboratories

Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles.

Zeneca Pharmaceuticals

A novel class of cyclic beta-dicarbonyl leaving groups and their use in the design of benzisothiazolone human leukocyte elastase inhibitors.

Sterling Winthrop Pharmaceuticals Research Division

Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.

Eli Lilly

On the Process of Discovering Leads That Target the Heparin-Binding Site of Neutrophil Elastase in the Sputum of Cystic Fibrosis Patients.

Virginia Commonwealth University

Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin.

TBA

Three-dimensional quantitative structure-activity relationship analyses using comparative molecular field analysis and comparative molecular similarity indices analysis to elucidate selectivity differences of inhibitors binding to trypsin, thrombin, and factor Xa.

University of Marburg

Substituted 2-pyrones, 2-pyridones, and other congeners of elasnin as potential agents for the treatment of chronic obstructive lung diseases.

TBA

Amino acid derived latent isocyanates: irreversible inactivation of porcine pancreatic elastase and human leukocyte elastase.

TBA

1H-pyrrolo[2,3-b]pyridine: A new scaffold for human neutrophil elastase (HNE) inhibitors.

University of Florence

A BODIPY-Tagged Phosphono Peptide as Activity-Based Probe for Human Leukocyte Elastase.

University of Bonn

Inhibition of human sputum elastase by substituted 2-pyrones.

TBA

Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs.

University of Nottingham

(Acyloxy)benzophenones and (acyloxy)-4-pyrones. A new class of inhibitors of human neutrophil elastase.

Searle Research and Development

Probing the Antiallergic and Anti-inflammatory Activity of Biflavonoids and Dihydroflavonols from Dietes bicolor.

Ain Shams University

Inhibition of human leukocyte elastase. 3. Synthesis and activity of 3'-substituted cephalosporins.

Merck Sharp and Dohme Research Laboratories

Inhibition of human leukocyte elastase. 2. Inhibition by substituted cephalosporin esters and amides.

Merck Sharp and Dohme Research Laboratories

Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters.

Merck Sharp and Dohme Research Laboratories

Potential Anti-inflammatory Effects of the Fruits of Paulownia tomentosa.

Korea Research Institute of Bioscience and Biotechnology

Synthesis of peptidyl fluoromethyl ketones and peptidyl alpha-keto esters as inhibitors of porcine pancreatic elastase, human neutrophil elastase, and rat and human neutrophil cathepsin G.

Merrell Dow Research Institute

Design of Potent and Selective Cathepsin G Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold.

The University of Queensland

Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry.

St. John'S University

Inhibition of human leukocyte elastase by N-substituted peptides containing alpha,alpha-difluorostatone residues at P1.

Boehringer Ingelheim Pharmaceuticals

Synthesis, antielastase, antioxidant and radical scavenging activities of 4-(aza substituted) methylene substituted dihydroxy coumarines.

Giresun University

Polyphenol fatty acid esters as serine protease inhibitors: a quantum-chemical QSAR analysis.

Slovak University of Technology

Synthesis, stability, biochemical and pharmacokinetic properties of a new potent and selective 4-oxo-ß-lactam inhibitor of human leukocyte elastase.

University of Lisbon

Potential of pyrazolooxadiazinone derivatives as serine protease inhibitors.

UniversitÀ

Development of a highly water-soluble peptide-based human neutrophil elastase inhibitor; AE-3763 for treatment of acute organ injury.

Dainippon Sumitomo Pharma

Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase.

Curacyte Chemistry

N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase.

Montana State University

Design and synthesis of novel and potent inhibitors of the type II transmembrane serine protease, matriptase, based upon the sunflower trypsin inhibitor-1.

Georgetown University Medical Center