Indole-2-carboxamide-based MmpL3 Inhibitors Show Exceptional Antitubercular Activity in an Animal Model of Tuberculosis Infection

Journal of Medicinal Chemistry

Volumn 59, Issue 13, 2016, Pages 6232-6247

  Stec, Jozef ^d,e   Onajole, Oluseye K ^a,f   Lun, Shichun ^b   Guo, Haidan ^b   Merenbloom, Benjamin ^b   Vistoli, Giulio ^g   Bishai, William R ^b,c   Kozikowski, Alan P ^a  

^a UNIVERSITY OF ILLINOIS AT CHICAGO   (United States)

^b JOHNS HOPKINS UNIVERSITY SCHOOL OF MEDICINE   (United States)

^c HOWARD HUGHES MEDICAL INSTITUTE   (United States)

^d CHICAGO STATE UNIVERSITY   (United States)

^e MARSHALL B KETCHUM UNIVERSITY   (United States)

^f ROOSEVELT UNIVERSITY   (United States)

^g UNIVERSITY OF MILAN   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINO N CYCLOOCTYL 1H INDOLE 2 CARBOXAMIDE; 4,6 DICHLORO N (2,3 DIHYDRO 1H INDEN 2 YL) 1H INDOLE 2 CARBOXAMIDE; 4,6 DICHLORO N (ENDO 1,7,7 TRIMETHYLBICYCLO[2.2.1]HEPTAN 2YL) 1H INDOLE 2 CARBOXAMIDE; 4,6 DICHLORO N CYCLOOCTYL 1H INDOLE 2 CARBOXAMIDE; 4,6 DICHLORO N HEPTYL 1H INDOLE 2 CARBOXAMIDE; 4,6 DICHLORO N OCTYL 1H INDOLE 2 CARBOXAMIDE; 4,6 DICHLORO N [2,6,6 TRIMETHYLBICYCLO[3.1.1]HEPTAN 3 YL] 1H INDOLE 2 CARBOXAMIDE; 4,6 DIFLUORO N [2,6,6 TRIMETHYLBICYCLO[3.1.1]HEPTAN 3 YL]1H INDOLE 2 CARBOXAMIDE; 4,6 DIFUORO N [2,6,6 TRIMETHYLBICYCLO[3.1.1]HEPTAN 3 YL] 1H INDOLE 2 CARBOXAMIDE; 5 AMINO N CYCLOOCTYL 1H INDOLE 2 CARBOXAMIDE; 6 BROMO N CYCLOOCTYL 1H INDOLE 2 CARBOXAMIDE; AMIDE; INDOLE DERIVATIVE; N (1 ADAMANTANYL) 4,6 DICHLORO 1H INDOLE 2 CARBOXAMIDE; N (1 ADAMANTANYL) 6 BROMO 1H INDOLE 2 CARBOXAMIDE; N (1 CYCLOHEXYLETHYL) 4,6 DICHLORO 1H INDOLE 2 CARBOXAMIDE; N (1 CYCLOHEXYLETHYL) 4,6 DIFLUORO 1H INDOLE 2 CARBOXAMIDE; N (EXO BICYCLO[2.2.1]HEPTAN 2 YL) 4,6 DICHLORO 1H INDOLE 2 CARBOXAMIDE; N CYCLOHEPTYL 4 METHYL 1H INDOLE 2 CARBOXAMIDE; N CYCLOHEPTYL 4,6 DIMETHOXY 1H INDOLE 2 CARBOXAMIDE; N CYCLOHEPTYL 5 METHYL 1H INDOLE 2 CARBOXAMIDE; N CYCLOHEPTYL 5,7 DIMETHYL 1H INDOLE 2 CARBOXAMIDE; N CYCLOHEPTYL 7 METHYL 1H INDOLE 2 CARBOXAMIDE; N CYCLOOCTYL 4,6 DIMETHOXY 1H INDOLE 2 CARBOXAMIDE; N CYCLOOCTYL 5 METHYL 1H INDOLE 2 CARBOXAMIDE; N CYCLOOCTYL 5,7 DIMETHYL 1H INDOLE 2 CARBOXAMIDE; N CYCLOOCTYL 6 METHYL 1H INDOLE 2 CARBOXAMIDE; RIFAMPICIN; TUBERCULOSTATIC AGENT; UNCLASSIFIED DRUG; UNINDEXED DRUG; BACTERIAL PROTEIN; CARRIER PROTEIN; MMPL3 PROTEIN, MYCOBACTERIUM TUBERCULOSIS;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; COLONY FORMING UNIT; COMPARATIVE STUDY; CONTROLLED STUDY; CYCLIZATION; DRUG BIOAVAILABILITY; FEMALE; HUMAN; HUMAN CELL; HYDROGENATION; HYDROLYSIS; IN VITRO STUDY; LIPOPHILICITY; LIQUID CHROMATOGRAPHY; LUNG TUBERCULOSIS; LUNG WEIGHT; MAMMAL CELL; MASS SPECTROMETRY; MEAN RESIDENCE TIME; MINIMUM INHIBITORY CONCENTRATION; MOLECULAR DOCKING; MONOTHERAPY; MOUSE; MYCOBACTERIUM TUBERCULOSIS; NONHUMAN; RAT; SELECTIVITY INDEX; SINGLE DRUG DOSE; SPLEEN WEIGHT; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION; VERO CELL LINE; ANIMAL; ANTAGONISTS AND INHIBITORS; BAGG ALBINO MOUSE; CHEMISTRY; DISEASE MODEL; DRUG DESIGN; DRUG EFFECTS; METABOLISM; MICROBIAL SENSITIVITY TEST; MICROBIOLOGY; MOLECULAR MODEL; MOLECULARLY TARGETED THERAPY; TUBERCULOSIS; TUBERCULOSIS, MULTIDRUG-RESISTANT;

ANIMALS; ANTITUBERCULAR AGENTS; BACTERIAL PROTEINS; DISEASE MODELS, ANIMAL; DRUG DESIGN; FEMALE; HUMANS; INDOLES; MEMBRANE TRANSPORT PROTEINS; MICE, INBRED BALB C; MICROBIAL SENSITIVITY TESTS; MODELS, MOLECULAR; MOLECULAR DOCKING SIMULATION; MOLECULAR TARGETED THERAPY; MYCOBACTERIUM TUBERCULOSIS; TUBERCULOSIS; TUBERCULOSIS, MULTIDRUG-RESISTANT;

EID: 84978648886     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.6b00415     Document Type: Article

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