Design and synthesis of conformationally restricted inhibitors of active thrombin activatable fibrinolysis inhibitor (TAFIa)

Bioorganic and Medicinal Chemistry

Volumn 22, Issue 7, 2014, Pages 2261-2268

  Brink, Mikael ^a   Dahlén, Anders ^a   Olsson, Thomas ^a   Polla, Magnus ^a   Svensson, Tor ^a  

^a ASTRAZENECA R AND D   (Sweden)

Author keywords

AstraZeneca; Carboxypeptidase U; Conformational restriction; Imidazole; Rigidification; TAFIa

Indexed keywords

4,5,6,7 TETRAHYDRO 1H BENZIMIDAZOLE 5 CARBOXYLIC ACID DERIVATIVE; 5 (3 AMINOPROPYL) 1 (3 METHYLBUTYL) 4,5,6,7 TETRAHYDRO 1H BENZIMIDAZOLE 5 CARBOXYLIC ACID; 5 (3 AMINOPROPYL) 1 (BIPHENYL 3 YLMETHYL) 4,5,6,7 TETRAHYDRO 1H BENZIMIDAZOLE 5 CARBOXYLIC ACID; 5 (3 AMINOPROPYL) 1 CYCLOHEXYL 4,5,6,7 TETRAHYDRO 1H BENZIMIDAZOLE 5 CARBOXYLIC ACID; 5 (3 AMINOPROPYL) 1 PHENYL 4,5,6,7 TETRAHYDRO 1H BENZIMIDAZOLE 5 CARBOXYLIC ACID; 5 (3 AMINOPROPYL) 1 PROPYL 4,5,6,7 TETRAHYDRO 1H BENZIMIDAZOLE 5 CARBOXYLIC ACID; 5 (3 AMINOPROPYL) 1 [2 [1,1' BI(CYCLOHEXYL) 4 YL]ETHYL] 4,5,6,7 TETRAHYDRO 1H BENZIMIDAZOLE 5 CARBOXYLIC ACID; 5,6,7,8 TETRAHYDROIMIDAZO[1,2 A]PYRIDINE 7 CARBOXYLIC ACID DERIVATIVE; 7 (2 AMINOPROPYL) 3 (2',4' DICHLOROBIPHENYL 3 YL) 5,6,7,8 TETRAHYDROIMIDAZO[1,2 A]PYRIDINE 7 CARBOXYLIC ACID; 7 (3 AMINOPROPYL) 3 ETHYL 5,6,7,8 TETRAHYDROIMIDAZO[1,2 A]PYRIDINE 7 CARBOXYLIC ACID; 7 (3 AMINOPROPYL) 3 PHENYL 5,6,7,8 TETRAHYDROIMIDAZO[1,2 A]PYRIDINE 7 CARBOXYLIC ACID; CARBOXYLIC ACID DERIVATIVE; THROMBIN ACTIVATABLE FIBRINOLYSIS INHIBITOR; UNCLASSIFIED DRUG; BENZIMIDAZOLE DERIVATIVE; ENZYME INHIBITOR; PYRIDINE DERIVATIVE;

ALKYLATION; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG CONFORMATION; DRUG DESIGN; DRUG PENETRATION; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; HYDROGENATION; IC 50; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; TIME TO MAXIMUM PLASMA CONCENTRATION; ANTAGONISTS AND INHIBITORS; CACO 2 CELL LINE; CHEMICAL STRUCTURE; CHEMISTRY; CONFORMATION; DOSE RESPONSE; GENETICS; HUMAN; METABOLISM; SYNTHESIS; X RAY CRYSTALLOGRAPHY;

BENZIMIDAZOLES; CACO-2 CELLS; CARBOXYPEPTIDASE B2; CRYSTALLOGRAPHY, X-RAY; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; ENZYME INHIBITORS; HUMANS; MODELS, MOLECULAR; MOLECULAR CONFORMATION; PYRIDINES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84897464175     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2014.02.010     Document Type: Article

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