195 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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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
Neutrophil elastase inhibitors for the treatment of (cardio)pulmonary diseases: Into clinical testing with pre-adaptive pharmacophores.
Bayer Healthcare
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)
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
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
N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases.
University Of Lisbon
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
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
Development of orally active nonpeptidic inhibitors of human neutrophil elastase.
Cortech
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
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
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
Design of alternate substrate inhibitors of serine proteases. Synergistic use of alkyl substitution to impede enzyme-catalyzed deacylation.
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
Tricyclic cephems as inhibitors of human leukocyte elastase. thieno[3,4-c]cepham sulfones and pyrrolo[3,4-c]cepham sulfones
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
Enantioselective synthesis and antielastase activity of 1,3,4-trisubstituted and 3,4-disubstituted β-lactam antibiotics
TBA
Inhibition of human leukocyte elastase. 5. Inhibition by 6-alkyl substituted penem benzyl esters.
TBA
Cephem sulfones as inactivators of human leukocyte elastase. II. Keto-enol tautomerish in cephem-4-ketones.
TBA
The effect of N-acyl substituents on the stability of monocyclic β-lactam inhibitors of human leukocyte elastase
TBA
Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2H)-one 1,1-dioxides.
University Of Leipzig
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
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)
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
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
Lung Protection by Cathepsin C Inhibition: A New Hope for COVID-19 and ARDS?
Centre D'Etude Des Pathologies Respiratoires And Universit£
Facile Synthesis of Aminomethyl Phosphinate Esters as Serine Protease Inhibitors with Primed Site Interaction.
Ku Leuven
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
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
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
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)
Preparation of alpha-keto ester enol acetates as potential prodrugs of human neutrophil elastase inhibitors.
Cinc
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)
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
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 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
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
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
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
(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
Inhibition of human leukocyte elastase by N-substituted peptides containing alpha,alpha-difluorostatone residues at P1.
Boehringer Ingelheim Pharmaceuticals
Synthesis and anticholinesterase activity of new substituted benzo[d]oxazole-based derivatives.
Shahid Bahonar University Of Kerman
Design, synthesis, and anticonvulsant activity of some derivatives of xanthone with aminoalkanol moieties.
Jagiellonian University Medical College
Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.
Pfizer
The pharmacological profile of (R)-3,4-dihydro-N-isopropyl-3-(N-isopropyl-N-propylamino)-2H-1-benzopyran-5-carboxamide, a selective 5-hydroxytryptamine(1A) receptor agonist.
Astrazeneca R&D
Structure-based design, synthesis, evaluation, and crystal structures of transition state analogue inhibitors of inosine monophosphate cyclohydrolase.
The Scripps Research Institute