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The European respiratory journal, ISSN 0903-1936, 10/2018, Volume 52, Issue 4
Journal Article
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 05/2018, Volume 26, Issue 8, pp. 1797 - 1809
Replacing the naphthalene C-unit of the anti-tuberculosis drug bedaquiline with a range of bicyclic heterocycles of widely differing lipophilicity gave analogs... 
Bedaquiline analogs | Tuberculosis | Drug development | Bedaquiline | MYCOBACTERIUM-TUBERCULOSIS | CHEMISTRY, MEDICINAL | DIARYLQUINOLINES | ASSAY | BIOCHEMISTRY & MOLECULAR BIOLOGY | MULTIDRUG-RESISTANT TUBERCULOSIS | CHEMISTRY, ORGANIC | Antitubercular agents | International cooperation | Research institutes | Drug therapy
Journal Article
LANCET INFECTIOUS DISEASES, ISSN 1473-3099, 02/2019, Volume 19, Issue 2, pp. 135 - 136
Journal Article
European Respiratory Journal, ISSN 0903-1936, 09/2016, Volume 48, Issue 3, pp. 938 - 943
The World Health Organization (WHO) estimated that 480000 new multidrug-resistant (MDR) tuberculosis (TB) cases occurred globally in 2014, with 190000 deaths.... 
BEDAQUILINE | DELAMANID | RESPIRATORY SYSTEM | DISEASE
Journal Article
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, ISSN 0066-4804, 10/2019, Volume 63, Issue 10
The antituberculosis drug bedaquiline (BDQ) inhibits Mycobacterium tuberculosis F-ATP synthase by interfering with two subunits. Drug binding to the c subunit... 
SYSTEM | diarylquinoline | MECHANISM | ANALOGS | DRUG BEDAQUILINE | MICROBIOLOGY | ADENOSINE-TRIPHOSPHATASE | c subunit | epsilon subunit | IDENTIFICATION | bedaquiline | TBAJ-876 | DIARYLQUINOLINES | F-ATP synthase | RESISTANCE | PHARMACOLOGY & PHARMACY
Journal Article
Journal of Pharmaceutical and Biomedical Analysis, ISSN 0731-7085, 11/2019, Volume 176, p. 112775
This article describes the simultaneous determination of bedaquiline fumarate (TMC-207) and rifabutin in human plasma by stable isotope dilution tandem mass... 
TMC-207 | Mycobacterium tuberculosis | Stable isotope dilution tandem mass spectrometry | Rifabutuin | Bedaquiline | 25-O-Desacetylrifabutin | Bedaquiline metabolite M2 | CHEMISTRY, ANALYTICAL | DIARYLQUINOLINES | ATP SYNTHASE | PHARMACOLOGY & PHARMACY
Journal Article
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 04/2019, Volume 27, Issue 7, pp. 1283 - 1291
The ATP-synthase inhibitor bedaquiline is effective against drug-resistant tuberculosis but is extremely lipophilic (clogP 7.25) with a very long plasma... 
Tuberculosis | Drug development | Bedaquiline analogues | Lipophilicity | Bedaquiline | CHEMISTRY, MEDICINAL | DIARYLQUINOLINES | ASSAY | BIOCHEMISTRY & MOLECULAR BIOLOGY | MULTIDRUG-RESISTANT TUBERCULOSIS | CHEMISTRY, ORGANIC | TMC207 | Drug resistance in microorganisms | Plasma physics | International cooperation | Pyridine | Pharmacy | Research institutes | Drug therapy
Journal Article
Clinical Pharmacology in Drug Development, ISSN 2160-763X, 05/2019, Volume 8, Issue 4, pp. 436 - 442
There is an urgent need to identify safe and effective combination treatments for multidrug‐resistant (MDR) Mycobacterium tuberculosis infection (TB).... 
pharmacokinetics | bedaquiline metabolites | bedaquiline | rifabutin | rifampin | PHARMACOLOGY & PHARMACY | PHARMACODYNAMICS | RIFAPENTINE | TMC207
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 02/2018, Volume 61, Issue 3, pp. 791 - 803
Inhibition of the mycolic acid pathway has proven a viable strategy in antitubercular drug discovery. The AccA3/AccD4/FadD32/Pks13 complex of Mycobacterium... 
PKS13 | BEDAQUILINE | DELAMANID | CHEMISTRY, MEDICINAL | CATALYZES | MYCOLIC ACID BIOSYNTHESIS | MEMBRANE | RECEPTOR | DIARYLQUINOLINE
Journal Article
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 10/2017, Volume 8, Issue 10, pp. 1019 - 1024
Bedaquiline (1) is a new drug for tuberculosis and the first of the diarylquinoline class. It demonstrates excellent efficacy against TB but induces... 
lipophilicity | ATP synthase | diarylquinoline | hERG | Bedaquiline | tuberculosis | DRUG | CHEMISTRY, MEDICINAL | TMC207
Journal Article
CLINICAL INFECTIOUS DISEASES, ISSN 1058-4838, 10/2019, Volume 69, Issue 7, pp. 1229 - 1231
Two new drugs, delamanid and bedaquiline, have recently been approved for treatment of multidrug-resistant and extensively drug-resistant (XDR) tuberculosis.... 
INFECTIOUS DISEASES | MICROBIOLOGY | IMMUNOLOGY | bedaquiline resistance | XDR-tuberculosis | delamanid resistance
Journal Article
Tuberculosis, ISSN 1472-9792, 07/2019, Volume 117, pp. 79 - 84
Bedaquiline was approved by USFDA in 2012 for pulmonary MDR-TB. The IC value of bedaquiline was reported to be remarkably low (25 nM), effectively inhibiting... 
Hepatotoxicity | Bedaquiline | Cardiotoxicity | ANALOGS | DRUG BEDAQUILINE | MICROBIOLOGY | IMMUNOLOGY | DISCOVERY | DIARYLQUINOLINES | ATP SYNTHASE | RESPIRATORY SYSTEM | MULTIDRUG-RESISTANT TUBERCULOSIS | TMC207 | Analysis | Tuberculosis | Organic chemistry | ATP synthase | Toxicity | Liver | Chemists | Inhibition | Pharmacokinetics | Potassium | Optimization
Journal Article
Antimicrobial Agents and Chemotherapy, ISSN 0066-4804, 07/2019, Volume 63, Issue 10
ABSTRACT The antituberculosis drug bedaquiline (BDQ) inhibits Mycobacterium tuberculosis F-ATP synthase by interfering with two subunits. Drug binding to the c... 
Journal Article
JOURNAL OF MEDICINAL CHEMISTRY, ISSN 0022-2623, 04/2019, Volume 62, Issue 7, pp. 3575 - 3589
Our group recently reported the identification of novel coumestan derivatives as Mycobacterium tuberculosis (Mtb) Pks13-thioesterase (TE) domain inhibitors,... 
PKS13 | BEDAQUILINE | DELAMANID | CHEMISTRY, MEDICINAL | ASSAY | CATALYZES | MYCOLIC ACID BIOSYNTHESIS | INHA
Journal Article
European Journal of Medicinal Chemistry, ISSN 0223-5234, 11/2019, Volume 182, p. 111644
The emergence of drug resistance in infectious microbial strains can be overcome by development of novel drug molecules against unexploited microbial target.... 
Antimicrobial | Oligomycin | Aurovertin | Peptides | Sesquiterpenes | Bedaquiline | Polyphenols | Steroidal alkaloids | FoF1 ATP synthase inhibitor | Heterocyclic
Journal Article
Emerging Infectious Diseases, ISSN 1080-6040, 10/2017, Volume 23, Issue 10, pp. 1718 - 1721
Journal Article
by Li, CG and Tang, YX and Sang, ZT and Yang, Y and Gao, YM and Yang, T and Fang, CT and Zhang, TY and Luo, YF
MEDCHEMCOMM, ISSN 2040-2503, 09/2019, Volume 10, Issue 9, pp. 1635 - 1640
Tuberculosis is the contagious disease responsible for the highest number of deaths worldwide. Here, we screened a commercially available compound library and... 
BEDAQUILINE | CHEMISTRY, MEDICINAL | CANCER | BIOCHEMISTRY & MOLECULAR BIOLOGY | DRUGS
Journal Article
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