166 articles for thisTarget

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PMID	Data	Article Title	Organization
28621538	63	Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.	Novartis Pharma
28157311	11	Structure-Based Library Design and Fragment Screening for the Identification of Reversible Complement Factor D Protease Inhibitors.	Novartis Institutes For Biomedical Research
27564532	3	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
26358162	27	Neutrophil elastase inhibitors for the treatment of (cardio)pulmonary diseases: Into clinical testing with pre-adaptive pharmacophores.	Bayer Healthcare
25782055	9	Discovery of a Cyclic Boronic Acidß-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.	Rempex Pharmaceuticals
25650311	76	Synthesis and pharmacological characterization of 2-aminobenzaldehyde oxime analogs as dual inhibitors of neutrophil elastase and proteinase 3.	Chang Gung University
25408826	8	Neutrophil elastase inhibitors as potential anti-inflammatory therapies.	Therachem Research Medilab (India)
915907	6	Proteinase inhibitors. I. Inhibitors of elastase.	TBA
24556381	4	Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase.	Universidad De Buenos Aires
24224573	31	Optimization of O3-acyl kojic acid derivatives as potent and selective human neutrophil elastase inhibitors.	Universidade De Lisboa
24135727	7	Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors.	Emory University
24102612	105	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
23844670	52	Optimization of N-benzoylindazole derivatives as inhibitors of human neutrophil elastase.	Universit£
23719288	41	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
23350733	10	Potent elastase inhibitors from cyanobacteria: structural basis and mechanisms mediating cytoprotective and anti-inflammatory effects in bronchial epithelial cells.	University Of Florida
2299617	173	Design and synthesis of 4H-3,1-benzoxazin-4-ones as potent alternate substrate inhibitors of human leukocyte elastase.	Syntex Research
4068006	46	Inhibition of human leukocyte elastase, porcine pancreatic elastase, and chymotrypsin by elasnin and other 4-hydroxy-2-pyrones.	TBA
21413808	170	Synopsis of some recent tactical application of bioisosteres in drug design.	Bristol-Myers Squibb Pharmaceutical Research And Development
22882079	26	Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.	Aarhus University
22595175	18	N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases.	University Of Lisbon
17535802	91	Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.	Merck Research Laboratories
18318470	1	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
18078761	2	Bornyl (3,4,5-trihydroxy)-cinnamate--an optimized human neutrophil elastase inhibitor designed by free energy calculations.	Albert-Ludwigs-University Of Freiburg
18053726	364	Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.	Johnson & Johnson Pharmaceutical Research & Development
18290604	1	Azetidine-2,4-diones (4-oxo-beta-lactams) as scaffolds for designing elastase inhibitors.	Universidade De Lisboa
18247547	6	Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.	Cephalon
17470393	6	Resisting degradation by human elastase: commonality of design features shared by 'canonical' plant and bacterial macrocyclic protease inhibitor scaffolds.	Imperial College
16078825	8	Design and synthesis of depeptidized macrocyclic inhibitors of hepatitis C NS3-4A protease using structure-based drug design.	Schering-Plough Research Institute
12190311	37	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
11312926	39	Development of orally active nonpeptidic inhibitors of human neutrophil elastase.	Cortech
10669559	180	Protease inhibitors: current status and future prospects.	University Of Queensland
9191965	58	Discovery and biological activity of orally active peptidyl trifluoromethyl ketone inhibitors of human neutrophil elastase.	Zeneca Pharmaceuticals
7799404	22	Inhibition of human neutrophil elastase with peptidyl electrophilic ketones. 2. Orally active PG-Val-Pro-Val pentafluoroethyl ketones.	Marion Merrell Dow Research Institute
8064791	18	2,6-Disubstituted aryl carboxylic acids, leaving groups"par excellence" for benzisothiazolone inhibitors of human leukocyte elastase.	Sterling Winthrop Pharmaceutical Research Division
1578486	53	Novel anthraquinone inhibitors of human leukocyte elastase and cathepsin G.	Georgia Institute Of Technology
1542092	38	Inhibition of human leukocyte elastase (HLE) by N-substituted peptidyl trifluoromethyl ketones.	Boehringer Ingelheim Pharmaceuticals
1433188	7	Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.	Merck Research Laboratories
11294386	5	The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate.	Glaxowellcome Medicines Research Centre
11206469	14	Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine-trans-lactams.	Glaxowellcome Medicines Research Centre
11055335	27	Highly potent and selective peptide-based inhibitors of the hepatitis C virus serine protease: towards smaller inhibitors.	Boehringer Ingelheim Pharmaceuticals
10360758	10	Metallopeptide approach to the design of biologically active ligands: design of specific human neutrophil elastase inhibitors.	Palatin Technologies
21923104	12	HLE-inhibitory alkaloids with a polyketide skeleton from the marine-derived fungus Coniothyrium cereale.	University Of Bonn
21741848	66	Design, synthesis and evaluation of N-benzoylindazole derivatives and analogues as inhibitors of human neutrophil elastase.	Universit£
20823284	9	Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.	Boehringer Ingelheim (Canada)
20970895	4	2-Azetidinone--a new profile of various pharmacological activities.	Barkatullah University
20638756	1	Inhibitors of human neutrophil elastase based on a highly functionalized N-amino-4-imidazolidinone scaffold.	Wichita State University
19841155	29	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.	Merck Research Laboratories
20417587	14	Synthesis and evaluation of benzoxazinone derivatives on activity of human neutrophil elastase and on hemorrhagic shock-induced lung injury in rats.	Chang Gung University
20102150	35	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
19772295	5	Potent inhibitors of beta-tryptase and human leukocyte elastase based on the MCoTI-II scaffold.	Imperial College
19665376	48	Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C.	Merck Frosst Canada
20004577	6	Evaluation of human neutrophil elastase inhibitory effect of iridoid glycosides from Hedyotis diffusa.	Korea Research Institute Of Bioscience And Biotechnology
19908842	84	Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.	National Human Genome Research Institute
19904934	31	4-Oxo-beta-lactams (azetidine-2,4-diones) are potent and selective inhibitors of human leukocyte elastase.	University Of Lisbon
19577470	49	Synthesis and optimization of 2-pyridin-3-yl-benzo[d][1,3]oxazin-4-one based inhibitors of human neutrophil elastase.	Activx Biosciences
3550086	31	Design of alternate substrate inhibitors of serine proteases. Synergistic use of alkyl substitution to impede enzyme-catalyzed deacylation.	TBA
	24	Inhibition of human cytomegalovirus protease by benzoxazinones and evidence of antiviral activity in cell culture	TBA
	5	Synthesis of 7α-methoxy-2-(1,3-dithiolan-2-ylidene)cephem sulphones. A new series of human leukocyte elastase inhibitors	TBA
	45	A comparative SAR and computer modeling study of benzisothiazolone, mechanism-based inhibitors with porcine pancreatic and human leukocyte elastase	TBA
	8	Tricyclic cephems as inhibitors of human leukocyte elastase. thieno[3,4-c]cepham sulfones and pyrrolo[3,4-c]cepham sulfones	TBA
	7	Tricyclic cephems as inhibitors of human leukocyte elastase. Furo[3,4-c]cepham sulfones	TBA
	55	The design of potent and stable benzisothiazolone inhibitors of human leukocyte elastase	TBA
	18	Inhibitors of human leukocyte elastase. 3.1 inhibition by tetrahydrobenzisothiazolinylmethyl aryl carboxylates	TBA
	14	Inhibitors of human leukocyte elastase. 2.1 synthesis and sar of benzisothiazolinylmethyl aryl ethers	TBA
	1	Phosphorous acid analogs of L-680,833, a potent monocyclic β-lactam inhibitor of human leukocyte elastase	TBA
	12	Alkoxy substituted benzisothiazolone (BIT) derivatives: potent inhibitors of human leukocyte elastase	TBA
	27	Synthesis and porcine pancreatic elastase inhibitory evaluation of 6α-(sulfonyl)oxy-and 6α-chloropenicillanate sulfone esters and 3α-(acyloxy)methyl-6α-chloropenam sulfones	TBA
	46	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
	2	Synthesis of new thiazinoindole derivatives and their evaluation as inhibitors of human leukocyte elastase and other related serine proteases	TBA
	18	Examination of peptidic α′,β-diamino-α,α-difluoroketones as inhibitors of human leukocyte elastase	TBA
	19	A benzisothiazolone class of potent, selective mechanism-based inhibitors of human leukocyte elastase	TBA
	4	elastase inhibitors containing conformationally restricted lactams as P3-P2 dipeptide replacements	TBA
	7	Janus compounds: dual inhibitors of proteinases	TBA
	30	Enantioselective synthesis and antielastase activity of 1,3,4-trisubstituted and 3,4-disubstituted β-lactam antibiotics	TBA
	6	Inhibition of human leukocyte elastase. 7. Inhibition by 6-substituted penicillin amides.	TBA
	32	Inhibition of human leukocyte elastase. 6. Inhibition by 6-substituted penicillin esters.	TBA
	18	Inhibition of human leukocyte elastase. 5. Inhibition by 6-alkyl substituted penem benzyl esters.	TBA
	17	Inhibition of human leukocyte elastase (HLE) by novel bicyclic β-lactams	TBA
	13	Cephem sulfones as inactivators of human leukocyte elastase. II. Keto-enol tautomerish in cephem-4-ketones.	TBA
	2	The effect of N-acyl substituents on the stability of monocyclic β-lactam inhibitors of human leukocyte elastase	TBA
	1	Potential mechanism-based inhibitors of proteolytic enzymes	TBA
	6	Synthesis of a peptidyl 2,2-difluoro-3-aminopropionate	TBA
	1	A general synthesis of 4-alkyl/aryl substituted saccharins	TBA
18701300	55	Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2H)-one 1,1-dioxides.	University Of Leipzig
17419055	30	Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors.	Daiichi Asubio Pharma
17145787	8	Cathepsin A is the major hydrolase catalyzing the intracellular hydrolysis of the antiretroviral nucleotide phosphonoamidate prodrugs GS-7340 and GS-9131.	Gilead Sciences
15588093	3	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)
12668020	29	Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.	3-Dimensional Pharmaceuticals
12565935	5	Synthesis and evaluation of delta-lactams (piperazones) as elastase inhibitors.	The Oxford Centre For Molecular Sciences And The Dyson Perrins Laboratory
12540231	39	Phenethyl amides as novel noncovalent inhibitors of hepatitis C virus NS3/4A protease: discovery, initial SAR, and molecular modeling.	Mrl Rome
12467634	67	3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors.	Currently Naeja Pharmaceutical
12372533	69	P1 Phenethyl peptide boronic acid inhibitors of HCV NS3 protease.	Bristol-Myers Squibb Pharmaceutical Research Institute
12161131	1	Clarification of mechanism of human sputum elastase inhibition by a new inhibitor, ONO-5046, using electrospray ionization mass spectrometry.	Minase Research Institute
11844670	27	Design and synthesis of peptide-based carboxylic acid-containing transition-state inhibitors of human neutrophil elastase.	Dainippon Pharmaceutical
11425539	23	Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.	Shionogi
11327591	1	Design, synthesis and stability of N-acyloxymethyl- and N-aminocarbonyloxymethyl-2-azetidinones as human leukocyte elastase inhibitors.	Ineti
11212109	14	The identification of alpha-ketoamides as potent inhibitors of hepatitis C virus NS3-4A proteinase.	Roche Discover Welwyn
11150162	15	Design and synthesis of new orally active nonpeptidic inhibitors of human neutrophil elastase.	Colorado State University
11078188	20	1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.	Shionogi
11078187	36	Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.	Shionogi
10866385	13	Mass spectrometry reveals elastase inhibitors from the reactive centre loop of alpha1-antitrypsin.	The Oxford Centre For Molecular Sciences
10639285	13	2-(diethylamino)thieno1,3??xazin-4-ones as stable inhibitors of human leukocyte elastase.	University Of Leipzig
10522707	16	2-chloro-3-substituted-1,4-naphthoquinone inactivators of human cytomegalovirus protease.	Glaxowellcome Medicines Research Centre
10476876	1	Molecular structure of FR901277, a novel inhibitor of human leukocyte elastase, and its binding mode simulation.	Fujisawa Pharmaceutical
10340616	6	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
9873654	37	5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.	Glaxo Wellcome Research And Development
9873610	48	Studies on the C-terminal of hexapeptide inhibitors of the hepatitis C virus serine protease.	Boehringer Ingelheim (Canada)
9871780	85	Inhibition of human cytomegalovirus protease N(o) with monocyclic beta-lactams.	Boehringer Ingelheim (Canada)
9871680	5	Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.	Proscript
9871629	6	Preparation of alpha-keto ester enol acetates as potential prodrugs of human neutrophil elastase inhibitors.	Cinc
9822554	14	1,2-Benzisothiazol-3-one 1,1-dioxide inhibitors of human mast cell tryptase.	Bristol-Myers Squibb Pharmaceutical Research Institute
9822552	2	Design and synthesis of hydrazinopeptides and their evaluation as human leukocyte elastase inhibitors.	Institut Jacques Monod (Umr Cnrs 7592/UniversitéS Paris Vi And Vii)
9767628	31	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
9667976	58	beta-Lactam derivatives as inhibitors of human cytomegalovirus protease.	Boehringer Ingelheim (Canada)
9651152	20	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
9572899	19	Novel thieno[2,3-d][1,3]oxazin-4-ones as inhibitors of human leukocyte elastase.	University Of Leipzig
9406601	109	Peptidomimetic inhibitors of the human cytomegalovirus protease.	Boehringer Ingelheim
9379436	46	Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase.	Zeneca Pharmaceuticals
9341917	69	7-alkylidenecephalosporin esters as inhibitors of human leukocyte elastase.	Southern Methodist University
9341916	30	Anionic- and lipophilic-mediated surface binding inhibitors of human leukocyte elastase.	RhôNe-Poulenc Rorer
9191969	31	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
8676347	39	Nonpeptidic inhibitors of human neutrophil elastase. 7. Design, synthesis, and in vitro activity of a series of pyridopyrimidine trifluoromethyl ketones.	Zeneca Pharmaceuticals
8176703	14	Design of orally active, non-peptidic inhibitors of human leukocyte elastase.	Zeneca Pharmaceuticals Group
7966161	45	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
7932559	42	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
7932558	30	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
7932532	23	Non-peptidic inhibitors of human leukocyte elastase. 1. The design and synthesis of pyridone-containing inhibitors.	Zeneca
7877139	8	Orally bioavailable benzisothiazolone inhibitors of human leukocyte elastase.	Sterling Winthrop
7837246	39	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
7837244	33	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
7837243	25	Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 2. Effect of varying the heterocyclic ring on in vitro potency.	Zeneca Pharmaceuticals
7837235	9	Nonpeptidic inhibitors of human leukocyte elastase. 6. Design of a potent, intratracheally active, pyridone-based trifluoromethyl ketone.	Zeneca Pharmaceuticals
7830264	16	Inhibition of human neutrophil elastase. 3. An orally active enol acetate prodrug.	Marion Merrell Dow Research Institute
7739015	12	Phosphonates and phosphinates: novel leaving groups for benzisothiazolone inhibitors of human leukocyte elastase.	Sterling Winthrop Pharmaceuticals Research Division
7629790	32	New orally active serine protease inhibitors.	Minase Research Institute
7608910	1	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
7562931	41	Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles.	Zeneca Pharmaceuticals
7473596	35	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
3848491	5	Substituted 2-pyrones, 2-pyridones, and other congeners of elasnin as potential agents for the treatment of chronic obstructive lung diseases.	TBA
3844034	13	Amino acid derived latent isocyanates: irreversible inactivation of porcine pancreatic elastase and human leukocyte elastase.	TBA
3647139	9	Inhibition of human sputum elastase by substituted 2-pyrones.	TBA
3361575	65	(Acyloxy)benzophenones and (acyloxy)-4-pyrones. A new class of inhibitors of human neutrophil elastase.	Searle Research And Development
2391693	17	Inhibition of human leukocyte elastase. 3. Synthesis and activity of 3'-substituted cephalosporins.	Merck Sharp And Dohme Research Laboratories
2391692	27	Inhibition of human leukocyte elastase. 2. Inhibition by substituted cephalosporin esters and amides.	Merck Sharp And Dohme Research Laboratories
2391691	55	Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters.	Merck Sharp And Dohme Research Laboratories
2296031	48	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
1479581	11	Inhibition of human leukocyte elastase by N-substituted peptides containing alpha,alpha-difluorostatone residues at P1.	Boehringer Ingelheim Pharmaceuticals
27863021	30	Synthesis and anticholinesterase activity of new substituted benzo[d]oxazole-based derivatives.	Shahid Bahonar University Of Kerman
27543433	6	Design, synthesis, and anticonvulsant activity of some derivatives of xanthone with aminoalkanol moieties.	Jagiellonian University Medical College
11714872	14	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
17324932	14	Structure-based design, synthesis, evaluation, and crystal structures of transition state analogue inhibitors of inosine monophosphate cyclohydrolase.	The Scripps Research Institute
7683725	30	5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.	Merck Research Laboratories