The 8-pyrrole-benzothiazinones are noncovalent inhibitors of DprE1 from Mycobacterium tuberculosis

Antimicrobial Agents and Chemotherapy

Volumn 59, Issue 8, 2015, Pages 4446-4452

  Makarov, Vadim ^a,b   Neres, João ^a,c,e   Hartkoorn, Ruben C ^a,c   Ryabova, Olga B ^a,b   Kazakova, Elena ^a,b   Šarkan, Michal ^a,d   Huszár, Stanislav ^a,d   Piton, Jérémie ^a,c   Kolly, Gaëlle S ^a,c   Vocat, Anthony ^a,c   Conroy, Trent M ^a,c   Mikušová, Katarína ^a,d   Cole, Stewart T ^a,c  

^a RUSSIAN ACADEMY OF SCIENCES   (Russian Federation)

^b BACH INSTITUTE OF BIOCHEMISTRY   (Russian Federation)

^c EPFL   (Switzerland)

^d Faculty of Natural Sciences   (Slovakia)

^e UCB PHARMA   (Belgium)

Author keywords

[No Author keywords available]

Indexed keywords

2 [2 METHYL 1,4 DIOXA 8 AZASPIRO [4,5]DEC 8 YL] 8 (1H PYRROL 1 YL) 6 (TRIFLUOROMETHYL) 4H 3 BENZOTHIAZIN 4 ONE; 2 [2 METHYL 1,4 DIOXA 8 AZASPIRO [4,5]DEC 8 YL] 8 NITRO 6 (TRIFLUOROMETHYL) 4H 1,3 BENZOTHIAZIN 4 ONE; 2 [4 (CYCLOHEXYLMETHYL) PIPERZIN 1 YL] 8 (1H PYRROL 1 YL) 6 (TRIFLUOROMETHYL) 4H 1,3 BENZOTHIAZIN 4 ONE; 2 [4 (CYCLOHEXYLMETHYL) PIPERZIN 1 YL] 8 (2,5 DIMETHYL 1H PYRROL 1 YL) 6 (TRIFLUOROMETHYL) 4H 1,3 BENZOTHIAZIN 4 ONE; BACTERIAL ENZYME; CARBAMAZEPINE; DECAPRENYLPHOSPHORYL BETA DEXTRO RIBOSE 2' OXIDASE; ISONIAZID; PYRROLE DERIVATIVE; TUBERCULOSTATIC AGENT; UNCLASSIFIED DRUG; 2-(2-METHYL-1,4-DIOXA-8-AZASPIRO(4.5)DEC-8-YL)-8-NITRO-6-(TRIFLUOROMETHYL)-4H-1,3-BENZOTHIAZIN-4-ONE; 2-PYRIDIN-2-YL-4H-1,3-BENZOTHIAZIN-4-ONE; 3-(6-(4-OXO-4H-1,3-BENZOTHIAZIN-2-YL)PYRIDIN-2-YL)PROPANOIC ACID; ALCOHOL DEHYDROGENASE; BACTERIAL PROTEIN; DPRE1 PROTEIN, MYCOBACTERIUM TUBERCULOSIS; PBTZ169; PIPERAZINE DERIVATIVE; PYRIDINE DERIVATIVE; SPIRO COMPOUND; THIAZINE DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIBIOTIC SENSITIVITY; ARTICLE; BACTERIAL STRAIN; BACTERICIDAL ACTIVITY; CONTROLLED STUDY; DRUG ABSORPTION; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG EXCRETION; DRUG METABOLISM; DRUG POTENCY; EPIMERIZATION; HUMAN; HUMAN CELL; IC50; IN VITRO STUDY; IN VIVO STUDY; INTRINSIC CLEARANCE; METABOLIC STABILITY; MINIMUM INHIBITORY CONCENTRATION; MOLECULAR MODEL; MOUSE; MYCOBACTERIUM BOVIS BCG; MYCOBACTERIUM SMEGMATIS; MYCOBACTERIUM TUBERCULOSIS; NONHUMAN; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION; ANIMAL; ANTAGONISTS AND INHIBITORS; BAGG ALBINO MOUSE; DISEASE MODEL; DRUG EFFECTS; ENZYME ACTIVE SITE; HEP-G2 CELL LINE; MALE; METABOLISM; MICROBIAL SENSITIVITY TEST; PROCEDURES; TUBERCULOSIS;

ALCOHOL OXIDOREDUCTASES; ANIMALS; ANTITUBERCULAR AGENTS; BACTERIAL PROTEINS; CATALYTIC DOMAIN; DISEASE MODELS, ANIMAL; HEP G2 CELLS; HUMANS; MALE; MICE; MICE, INBRED BALB C; MICROBIAL SENSITIVITY TESTS; MYCOBACTERIUM TUBERCULOSIS; PIPERAZINES; PYRIDINES; PYRROLES; SPIRO COMPOUNDS; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZINES; TUBERCULOSIS;

EID: 84939865012     PISSN: 00664804     EISSN: 10986596     Source Type: Journal    
DOI: 10.1128/AAC.00778-15     Document Type: Article

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