The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
10782685 |
9 |
Synthesis of a cyanopeptide-analogue with trypsin activating properties. |
Ernst-Moritz-Arndt-University |
23586812 |
38 |
Development of a selective peptide macrocycle inhibitor of coagulation factor XII toward the generation of a safe antithrombotic therapy. |
Ecole Polytechnique F�D�Rale De Lausanne Epfl |
23294255 |
114 |
Development of new cyclic plasmin inhibitors with excellent potency and selectivity. |
Philipps University Marburg |
10602702 |
22 |
Simple linear QSAR models based on quantum similarity measures. |
Czech Academy of Sciences |
22726924 |
14 |
Discovery of benzothiazole guanidines as novel inhibitors of thrombin and trypsin IV. |
Astrazeneca |
16250649 |
10 |
Selective inhibitors of the serine protease plasmin: probing the S3 and S3' subsites using a combinatorial library. |
Brown University |
14640539 |
112 |
Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1). |
Pharmaceutical Research Institute |
12930148 |
41 |
Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone. |
Johnson & Johnson Pharmaceutical Research & Development |
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 |
12036356 |
234 |
Design, synthesis, and activity of a novel series of factor Xa inhibitors: optimization of arylamidine groups. |
Berlex Biosciences |
12036355 |
36 |
Simple, intuitive calculations of free energy of binding for protein-ligand complexes. 1. Models without explicit constrained water. |
University of Parma |
10669559 |
180 |
Protease inhibitors: current status and future prospects. |
University of Queensland |
10956211 |
14 |
GRID/CPCA: a new computational tool to design selective ligands. |
Boehringer Ingelheim Pharma |
10425086 |
83 |
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1. |
Dupont Pharmaceuticals |
9464370 |
28 |
Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support. |
Merck Research Laboratories |
9083470 |
9 |
Design of highly potent noncovalent thrombin inhibitors that utilize a novel lipophilic binding pocket in the thrombin active site. |
Merck Research Laboratories |
9357536 |
47 |
Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P3 position. |
Merck Research Laboratories |
2319567 |
29 |
Analogues of 1,5-bis(4-amidinophenoxy)pentane (pentamidine) in the treatment of experimental Pneumocystis carinii pneumonia. |
University of North Carolina |
15081015 |
91 |
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors. |
The Bristol-Myers Squibb Pharmaceutical Research Institute |
12873514 |
56 |
Design and synthesis of potent and selective macrocyclic thrombin inhibitors. |
Merck Research Laboratories |
10698459 |
41 |
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: optimization of the S4 ligand. |
Dupont Pharmaceuticals |
10915051 |
43 |
The design and synthesis of thrombin inhibitors: analogues of MD805 containing non-polar surrogates for arginine at the P1 position. |
Novartis Horsham Research Centre |
10201829 |
9 |
1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors. |
Nv Organon |
10522702 |
26 |
Design, synthesis and testing of amino-bicycloaryl based orally bioavailable thrombin inhibitors. |
Nv Organon |
10498204 |
25 |
Aminoisoquinolines: design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA. |
Rh£Ne-Poulenc Rorer |
9873373 |
20 |
Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases). |
Institute For Drug Research |
| 24 |
L-373,890, An achiral, noncovalent, subnanomolar thrombin inhibitor |
TBA |
| 43 |
S1 heterocyclic thrombin inhibitors |
TBA |
19841155 |
29 |
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. |
Merck Research Laboratories |
| 15 |
Rational design, synthesis, and serine protease inhibitory activity of a novel P1-argininal derivative featuring a conformationally constrained P2–P3 bicyclic lactam moiety |
TBA |
| 37 |
Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitors |
TBA |
| 32 |
Bisbenzamidine isoxazoline derivatives as factor Xa inhibitors |
TBA |
| 27 |
Rational design and synthesis of a novel, selective class of thrombin inhibitors: P1-argininal derivatives incorporating P3---P4 quaternary lactam dipeptide surrogates |
TBA |
| 44 |
Biaryl substituted alkylboronate esters as thrombin inhibitors |
TBA |
| 3 |
An efficient preparation of the potent and selective pseudopeptide thrombin inhibitor, inogatran |
TBA |
| 25 |
Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogates |
TBA |
| 15 |
RATIONAL DESIGN, SYNTHESIS, AND SERINE PROTEASE INHIBITORY ACTIVITY OF NOVEL P1-ARGININOYL HETEROCYCLES |
TBA |
| 78 |
Synthesis and evaluation of 2-aryl-4H-3,1-benzoxazin-4-ones as C1r serine protease inhibitors |
TBA |
| 61 |
(N-acyl-N-alkyl)glycyl borolysine analogs: A new class of potent thrombin inhibitors |
TBA |
15801822 |
28 |
9-hydroxyazafluorenes and their use in thrombin inhibitors. |
Merck Research Laboratories |
15203158 |
84 |
Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa. |
Merck |
15149645 |
92 |
Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors. |
Abbott Laboratories |
15149641 |
44 |
A novel series of potent and selective small molecule inhibitors of the complement component C1s. |
3-Dimensional Pharmaceuticals |
15081014 |
35 |
Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase. |
The Bristol-Myers Squibb Pharmaceutical Research Institute |
15080981 |
72 |
N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors. |
Millennium Pharmaceuticals |
15013007 |
319 |
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity. |
Millennium Pharmaceuticals |
15013006 |
69 |
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs. |
Millennium Pharmaceuticals |
15006404 |
56 |
Thrombin inhibitors built on an azaphenylalanine scaffold. |
University of Ljubljana |
14980671 |
78 |
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors. |
Millennium Pharmaceuticals |
14980670 |
107 |
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs. |
Millennium Pharmaceuticals |
14761180 |
31 |
Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G. |
Johnson & Johnson Pharmaceutical Research & Development |
14711304 |
117 |
Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution. |
Abbott Laboratories |
14698147 |
60 |
Synthesis of potent and selective 2-azepanone inhibitors of human tryptase. |
The Bristol-Myers Squibb Pharmaceutical Research Institute |
14505652 |
45 |
Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position. |
Merck Research Laboratories |
12824026 |
14 |
Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex. |
Pharmacia |
12824020 |
31 |
Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives. |
Boehringer Ingelheim Pharma |
12668020 |
29 |
Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors. |
3-Dimensional Pharmaceuticals |
12668008 |
34 |
3-amino-4-sulfonylpyridinone acetamide and related pyridothiadiazine thrombin inhibitors. |
Merck Research Laboratories |
12643903 |
81 |
Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors. |
Bristol-Myers Squibb |
12639567 |
135 |
Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors. |
Millennium Pharmaceuticals |
12617893 |
28 |
Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors. |
Merck Research Laboratories |
12617892 |
43 |
Novel thrombin inhibitors incorporating non-basic partially saturated heterobicyclic P1-arginine mimetics. |
University of Ljubljana |
12593666 |
30 |
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor. |
Senju Pharmaceutical |
12593648 |
53 |
Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand. |
Aventis Pharmaceuticals |
12570369 |
60 |
Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines. |
Merck Research Laboratories |
12565931 |
37 |
Nonbenzamidine tetrazole derivatives as factor Xa inhibitors. |
Bristol-Myers Squibb |
12482444 |
38 |
Design and synthesis of factor Xa inhibitors and their prodrugs. |
Millennium Pharmaceuticals |
12113838 |
36 |
Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification. |
Millennium Pharmaceuticals |
12039587 |
39 |
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity. |
Aventis Pharmaceuticals |
12039586 |
42 |
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency. |
Aventis Pharmaceuticals |
12039584 |
59 |
Design, synthesis, and SAR of monobenzamidines and aminoisoquinolines as factor Xa inhibitors. |
Millennium Pharmaceuticals |
12039583 |
140 |
Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P(1) structure-activity relationships of the substituted 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides. |
Millennium Pharmaceuticals |
12036353 |
38 |
Design of selective thrombin inhibitors based on the (R)-Phe-Pro-Arg sequence. |
Pfizer |
12031331 |
48 |
Design, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors. |
Millennium Pharmaceuticals |
11965378 |
78 |
Benzimidazole-based fXa inhibitors with improved thrombin and trypsin selectivity. |
Berlex Biosciences |
11958994 |
31 |
Benzimidazoles and isosteric compounds as potent and selective factor Xa inhibitors. |
Aventis Pharmaceuticals |
11934589 |
57 |
Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates. |
Corvas International |
11844691 |
107 |
4-amidinobenzylamine-based inhibitors of urokinase. |
Universitat Jena |
11677132 |
65 |
Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors. |
Cor Therapeutics |
11527714 |
66 |
Design and synthesis of glycolic and mandelic acid derivatives as factor Xa inhibitors. |
Cor Therapeutics |
11527709 |
19 |
Optimization of a screening lead for factor VIIa/TF. |
Axys Pharmaceuticals |
11495587 |
198 |
Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa. |
Axys Pharmaceuticals |
11459634 |
94 |
Development of potent and selective factor Xa inhibitors. |
Axys Pharmaceuticals |
11378359 |
57 |
Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors. |
3-Dimensional Pharmaceuticals |
11266180 |
74 |
The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa. |
Prosthetics Molecular Design |
11212093 |
21 |
Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: transition state inhibitors. |
Biochem Pharma |
11087565 |
86 |
Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors. |
Dupont Pharmaceuticals |
11078188 |
20 |
1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma. |
Shionogi |
11063603 |
53 |
Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors. |
Pfizer |
11055356 |
236 |
Dibasic inhibitors of human mast cell tryptase. Part 2: structure-activity relationships and requirements for potent activity. |
Axys Pharmaceuticals |
11055355 |
72 |
Dibasic inhibitors of human mast cell tryptase. Part 1: synthesis and optimization of a novel class of inhibitors. |
Axys Pharmaceuticals |
11055344 |
37 |
Novel, potent and selective chimeric FXa inhibitors featuring hydrophobic P1-ketoamide moieties. |
Corvas International |
10937736 |
35 |
Nonbenzamidine compounds as selective factor Xa inhibitors. |
Aventis Pharmaceuticals |
10915052 |
20 |
The design and synthesis of thrombin inhibitors: the introduction of in vivo efficacy and oral bioavailability into benzthiazolylalanine inhibitors. |
Novartis Horsham Research Centre |
10866385 |
13 |
Mass spectrometry reveals elastase inhibitors from the reactive centre loop of alpha1-antitrypsin. |
The Oxford Centre For Molecular Sciences |
10853668 |
52 |
Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors. |
Berlex Biosciences |
27476144 |
94 |
Trypsin inhibitors for the treatment of pancreatitis. |
Novartis Pharma |
10843219 |
20 |
Bicyclic pyridones as potent, efficacious and orally bioavailable thrombin inhibitors. |
Merck Research Laboratories |
27347787 |
32 |
Macrocyclic Prodrugs of a Selective Nonpeptidic Direct Thrombin Inhibitor Display High Permeability, Efficient Bioconversion but Low Bioavailability. |
Astrazeneca |
10782677 |
73 |
Guanylpiperidine peptidomimetics: potent and selective bis-cation inhibitors of factor Xa. |
Corvas International |
10698439 |
68 |
Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa. |
Rhone-Poulenc Rorer |
10669563 |
7 |
Structural basis of the thrombin selectivity of a ligand that contains the constrained arginine mimic (2S)-2-amino-(3S)-3-(1-carbamimidoyl- piperidin-3-yl)-propanoic acid at P1. |
Warner-Lambert |
10617091 |
73 |
Exploratory solid-phase synthesis of factor Xa inhibitors: discovery and application of p3-heterocyclic amides as novel types of non-basic arginine surrogates. |
Corvas International |
10509929 |
116 |
Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors. |
RhôNe-Poulenc Rorer |
10498211 |
42 |
Novel benzo-fused lactam scaffolds as factor Xa inhibitors. |
Corvas International |
10498197 |
58 |
The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 2. |
Warner-Lambert |
10498196 |
42 |
The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 1. |
Warner-Lambert |
10425106 |
12 |
4-Heterocyclohexanone-based inhibitors of the serine protease plasmin. |
Brown University |
10425087 |
110 |
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2. |
Dupont Pharmaceuticals |
10397495 |
49 |
Thrombin inhibitors based on [5,5] trans-fused indane lactams. |
Glaxo Wellcome Research and Development |
10328312 |
27 |
Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa. |
Dupont Pharmaceuticals |
10328293 |
23 |
The discovery of orally available thrombin inhibitors: optimisation of the P1 pharmacophore. |
Novartis Horsham Research Centre |
10230612 |
22 |
Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors. |
Dupont Pharmaceuticals |
10206557 |
36 |
Investigation of the S3 site of thrombin: design, synthesis and biological activity of 4-substituted 3-amino-2-pyridones incorporating P1-argininals. |
Corvas International |
10206546 |
27 |
Potent and selective bicyclic lactam inhibitors of thrombin: Part 3: P1' modifications. |
Warner-Lambert |
10206542 |
50 |
Benzenesulfonamide derivatives of 2-substituted 4H-3,1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease. |
Warner-Lambert |
10091694 |
90 |
Symmetrical anhydride-type serine protease inhibitors: structure-activity relationship studies of human chymase inhibitors. |
Nippon Steel |
9934495 |
26 |
Alkoxide-catalyzed ring-opening of a novel homosaccharin derivative: synthesis of potent, selective P3-lactam thrombin inhibitors containing P4-o-alkoxycarbonylbenzylsulfonamide residues. |
Corvas International |
9873743 |
13 |
Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications. |
Warner-Lambert |
9873654 |
37 |
5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor. |
Glaxo Wellcome Research and Development |
9873607 |
21 |
The de novo design and synthesis of cyclic urea inhibitors of factor Xa: initial SAR studies. |
Dupont Pharmaceuticals |
9873569 |
16 |
Design and construction of novel thrombin inhibitors featuring P3-P4 quaternary lactam dipeptide surrogates. |
Corvas International |
9873535 |
13 |
Highly efficient and versatile synthesis of libraries of constrained beta-strand mimetics. |
Molecumetics |
9873422 |
16 |
C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption. |
Merck Research Laboratories |
9873418 |
16 |
Identification and SAR for a selective, nonpeptidyl thrombin inhibitor. |
Merck Research Laboratories |
9871547 |
15 |
L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor. |
Merck Research Laboratories |
9871540 |
100 |
Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors. |
Dupont Pharmaceuticals |
9804686 |
16 |
Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates. |
Merck Research Laboratories |
9703466 |
35 |
Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position. |
Merck Research Laboratories |
9438022 |
55 |
Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors. |
Dupont Pharmaceuticals |
9379436 |
46 |
Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase. |
Zeneca Pharmaceuticals |
9171866 |
12 |
Potent noncovalent thrombin inhibitors that utilize the unique amino acid D-dicyclohexylalanine in the P3 position. Implications on oral bioavailability and antithrombotic efficacy. |
Merck Research Laboratories |
8917639 |
50 |
Design, synthesis, and evolution of a novel, selective, and orally bioavailable class of thrombin inhibitors: P1-argininal derivatives incorporating P3-P4 lactam sulfonamide moieties. |
Corvas International |
8426361 |
111 |
Highly selective tripeptide thrombin inhibitors. |
Eli Lilly |
8035417 |
23 |
Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
7629790 |
32 |
New orally active serine protease inhibitors. |
Minase Research Institute |
7562936 |
10 |
Synthesis of tight binding inhibitors and their action on the proprotein-processing enzyme furin. |
Friedrich Miescher-Institut |
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 |
12061879 |
44 |
SMall Molecule Growth 2001 (SMoG2001): an improved knowledge-based scoring function for protein-ligand interactions. |
Harvard University |
29936356 |
27 |
Engineering potent mesotrypsin inhibitors based on the plant-derived cyclic peptide, sunflower trypsin inhibitor-1. |
The University of Queensland |
2136920 |
39 |
New leupeptin analogues: synthesis and inhibition data. |
University of Arkansas |
14744476 |
35 |
Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity. |
Emory University |
20626411 |
14 |
Fragment-based discovery of novel thymidylate synthase leads by NMR screening and group epitope mapping. |
University of Washington |
15713402 |
51 |
Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase. |
Bristol-Myers Squibb |
12657282 |
13 |
Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives. |
Abbott Laboratories |
24058293 |
12 |
Modulation of global low-frequency motions underlies allosteric regulation: demonstration in CRP/FNR family transcription factors. |
Durham University |
10715152 |
151 |
5,6-Dihydropyran-2-ones possessing various sulfonyl functionalities: potent nonpeptidic inhibitors of HIV protease. |
Parke-Davis Pharmaceutical Research |