Creating novel activated factor XI inhibitors through fragment based lead generation and structure aided drug design

PLoS ONE

Volumn 10, Issue 1, 2015, Pages

  Fjellström, Ola ^a   Akkaya, Sibel ^a   Beisel, Hans Georg ^a   Eriksson, Per Olof ^a   Erixon, Karl ^a   Gustafsson, David ^a   Jurva, Ulrik ^a   Kang, Daiwu ^a   Karis, David ^a   Knecht, Wolfgang ^a   Nerme, Viveca ^a   Nilsson, Ingemar ^a   Olsson, Thomas ^a   Redzic, Alma ^a   Roth, Robert ^a   Sandmark, Jenny ^a   Tigerström, Anna ^a   Öster, Linda ^a  

^a ASTRAZENECA R AND D   (Sweden)

Author keywords

[No Author keywords available]

Indexed keywords

2 (4 HYDROXY 2 OXO 1,2 DIHYDROQUINOLINE 6 CARBOXAMIDO) 3 PHENYLPROPANOIC ACID; 2 ACETAMIDO N [(6 CHLORO 2 OXO 1,2 DIHYDROQUINOLIN 4 YL)METHYL] 3 PHENYLPROPANAMIDE; 2 AMINO N [(6 CHLORO 2 OXO 1,2 DIHYDROQUINOLIN 4 YL)METHYL] 3 PHENYLPROPANAMIDE; 2 CHLORO 5 METHYLQUINOLINE; 3 (6 CHLORO 2 OXO 1,2 DIHYDROQUINOLIN 4 YL)PROPANOIC ACID; 3 ETHOXY N M TOLYLACRYLAMIDE; 4 (AMINOMETHYL) 6 CHLOROQUINOLIN 2(1H) ONE; 4 (BROMOMETHYL) 6 CHLOROQUINOLIN 2(1H) ONE; 4 BROMO N (4 CHLOROPHENYL) 3 OXOBUTANAMIDE; 4 HYDROXY 2 OXO 1,2 DIHYDROQUINOLINE 6 CARBOXYLIC ACID; 4 HYDROXY N (1 (METHYLAMINO) 1 OXO 3 PHENYLPROPAN 2 YL) 2 OXO 1,2 DIHYDROQUINOLINE 6 CARBOXAMIDE; 5 (AMINOMETHYL)QUINOLIN 2 AMINE; 5 METHYLQUINOLIN 2 AMINE; 5 METHYLQUINOLIN 2(1H) ONE; 6 CHLORO 3,4 DIHYDRO 1H QUINOLIN 2 ONE; BLOOD CLOTTING FACTOR 11; BLOOD CLOTTING INHIBITOR; DIETHYL 2 [(6 CHLORO 2 OXO 1,2 DIHYDROQUINOLIN 4 YL)METHYL]MALONIC ACID; N (1 (DIMETHYLAMINO) 1 OXO 3 PHENYLPROPAN 2 YL) 4 HYDROXY 2 OXO 1,2 DIHYDROQUINOLINE 6 CARBOXAMIDE; N (3 (2 (2 AMINOETHOXY)ETHOXY)PHENYL) 6 CARBAMIMIDOYL 4 (PYRIMIDIN 2 YLAMINO) 2 NAPHTHAMIDE; N (4 CHLOROPHENYL) 3 OXOBUTANAMIDE; N (5 (AMINOMETHYL)QUINOLIN 2 YL)ACETAMIDE; N (5 (AZIDOMETHYL)QUINOLIN 2 YL)ACETAMIDE; N (5 (BROMOMETHYL)QUINOLIN 2 YL)ACETAMIDE; N (5 METHYLQUINOLIN 2 YL)ACETAMIDE; N [1 [(2 AMINOQUINOLIN 5 YL)METHYLAMINO] 1 OXO 3 PHENYLPROPAN 2 YL] 4 HYDROXY 2 OXO 1,2 DIHYDROQUINOLINE 6 CARBOXAMIDE; N [1 [(6 CHLORO 2 OXO 1,2 DIHYDROQUINOLIN 4 YL)METHYLAMINO] 1 OXO 3 PHENYLPROPAN 2 YL] 4 HYDROXY 2 OXO 1,2 DIHYDROQUINOLINE 6 CARBOXAMIDE; QUINOLIN 2 AMINE; TERT BUTYL 1 [(6 CHLORO 2 OXO 1,2 DIHYDROQUINOLIN 4 YL)METHYLAMINO] 1 OXO 3 PHENYLPROPAN 2 YLCARBAMIC ACID; UNCLASSIFIED DRUG; UNINDEXED DRUG; BLOOD CLOTTING FACTOR 11A; LIGAND; PEPTIDE LIBRARY; PROTEIN BINDING; SERINE PROTEINASE INHIBITOR;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; BINDING SITE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG DISTRIBUTION; DRUG EXCRETION; DRUG METABOLISM; DRUG PENETRATION; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TRANSPORT; ENZYME INHIBITION ASSAY; FEMALE; HUMAN; HUMAN CELL; HYDROPHILICITY; MOLECULAR DOCKING; NONHUMAN; NUCLEAR MAGNETIC RESONANCE; PHYSICAL CHEMISTRY; RAT; REVIEW; SURFACE PLASMON RESONANCE; X RAY CRYSTALLOGRAPHY; AMINO ACID SEQUENCE; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; CHEMISTRY; CONFORMATION; MOLECULAR GENETICS; PEPTIDE LIBRARY; PRECLINICAL STUDY; PROCEDURES; QUANTITATIVE STRUCTURE ACTIVITY RELATION;

AMINO ACID SEQUENCE; BINDING SITES; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; FACTOR XIA; HUMANS; LIGANDS; MODELS, MOLECULAR; MOLECULAR CONFORMATION; MOLECULAR SEQUENCE DATA; NUCLEAR MAGNETIC RESONANCE, BIOMOLECULAR; PEPTIDE LIBRARY; PROTEIN BINDING; QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP; SERINE PROTEINASE INHIBITORS;

EID: 84961290331     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0113705     Document Type: Review

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