(6S)-2-nitro-6-{[4-(trifluoromethoxy)phenyl]methoxy}-5H,6H,7H-imidazo[2,1-b][1,3]oxazine
| Title | Journal |
|---|---|
| Pentacyclic nitrofurans with in vivo efficacy and activity against nonreplicating Mycobacterium tuberculosis. | PloS one 20140101 |
| Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis. | Journal of natural products 20131025 |
| Preliminary structure-activity relationships and biological evaluation of novel antitubercular indolecarboxamide derivatives against drug-susceptible and drug-resistant Mycobacterium tuberculosis strains. | Journal of medicinal chemistry 20130523 |
| 14-day bactericidal activity of PA-824, bedaquiline, pyrazinamide, and moxifloxacin combinations: a randomised trial. | Lancet (London, England) 20120915 |
| New drug combination for TB is tested in unique trial. | BMJ (Clinical research ed.) 20120725 |
| Tuberculosis: the drug development pipeline at a glance. | European journal of medicinal chemistry 20120501 |
| Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases. | Journal of medicinal chemistry 20120426 |
| Generation and exploration of new classes of antitubercular agents: The optimization of oxazolines, oxazoles, thiazolines, thiazoles to imidazo[1,2-a]pyridines and isomeric 5,6-fused scaffolds. | Bioorganic & medicinal chemistry 20120401 |
| Trial tests new combination of drugs to treat tuberculosis. | BMJ (Clinical research ed.) 20120320 |
| Identification, design and biological evaluation of heterocyclic quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2). | Journal of medicinal chemistry 20120308 |
| Synthesis and evaluation of anti-tubercular and antibacterial activities of new 4-(2,6-dichlorobenzyloxy)phenyl thiazole, oxazole and imidazole derivatives. Part 2. | European journal of medicinal chemistry 20120301 |
| Mouse model of necrotic tuberculosis granulomas develops hypoxic lesions. | The Journal of infectious diseases 20120215 |
| Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). | Journal of medicinal chemistry 20120112 |
| Structure of Ddn, the deazaflavin-dependent nitroreductase from Mycobacterium tuberculosis involved in bioreductive activation of PA-824. | Structure (London, England : 1993) 20120111 |
| Substrate specificity of the deazaflavin-dependent nitroreductase from Mycobacterium tuberculosis responsible for the bioreductive activation of bicyclic nitroimidazoles. | The FEBS journal 20120101 |
| Rapid evaluation in whole blood culture of regimens for XDR-TB containing PNU-100480 (sutezolid), TMC207, PA-824, SQ109, and pyrazinamide. | PloS one 20120101 |
| Integrative analysis of transcriptome and genome indicates two potential genomic islands are associated with pathogenesis of Mycobacterium tuberculosis. | Gene 20111201 |
| Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin. | Bioorganic & medicinal chemistry letters 20111015 |
| Synthesis and structure-activity relationships of varied ether linker analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5h-imidazo[2,1-b][1,3]oxazine (PA-824). | Journal of medicinal chemistry 20111013 |
| Pharmacophore modeling and density functional theory analysis for a series of nitroimidazole compounds with antitubercular activity. | Chemical biology & drug design 20110901 |
| Structure-activity relationships of antitubercular nitroimidazoles. 3. Exploration of the linker and lipophilic tail of ((s)-2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazin-6-yl)-(4-trifluoromethoxybenzyl)amine (6-amino PA-824). | Journal of medicinal chemistry 20110825 |
| The TB Alliance: overcoming challenges to chart the future course of TB drug development. | Future medicinal chemistry 20110801 |
| Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity. | European journal of medicinal chemistry 20110601 |
| Synthesis and antimycobacterial activities of non-purine analogs of 6-aryl-9-benzylpurines: Imidazopyridines, pyrrolopyridines, benzimidazoles, and indoles. | Bioorganic & medicinal chemistry 20110601 |
| Novel thiolactone-isatin hybrids as potential antimalarial and antitubercular agents. | Bioorganic & medicinal chemistry letters 20110401 |
| Synthesis and antitubercular activity of monocyclic nitroimidazoles: insights from econazole. | Bioorganic & medicinal chemistry letters 20110301 |
| The effect of 5-substitution on the electrochemical behavior and antitubercular activity of PA-824. | Bioorganic & medicinal chemistry letters 20110115 |
| Comparative bioactivation of the novel anti-tuberculosis agent PA-824 in Mycobacteria and a subcellular fraction of human liver. | British journal of pharmacology 20110101 |
| Half-century-old TB drugs get a facelift in new cocktails. | Nature medicine 20101201 |
| A concise and convergent synthesis of PA-824. | The Journal of organic chemistry 20101105 |
| Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring. | Bioorganic & medicinal chemistry 20101015 |
| The nitroimidazooxazines (PA-824 and analogs): structure-activity relationship and mechanistic studies. | Future medicinal chemistry 20100801 |
| Synthesis, antimalarial and antitubercular activity of acetylenic chalcones. | Bioorganic & medicinal chemistry letters 20100201 |
| Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains. | Journal of medicinal chemistry 20100128 |
| Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis. a potent and selective series for further drug development. | Journal of medicinal chemistry 20100128 |
| Release of nitrite from the antitubercular nitroimidazole drug PA-824 and analogues upon one-electron reduction in protic, non-aqueous solvent. | Organic & biomolecular chemistry 20100121 |
| Synthesis and structure-activity studies of biphenyl analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). | Journal of medicinal chemistry 20100114 |
| Discovery and development of the covalent hydrates of trifluoromethylated pyrazoles as riboflavin synthase inhibitors with antibiotic activity against Mycobacterium tuberculosis. | The Journal of organic chemistry 20090807 |
| Structure-activity relationships of antitubercular nitroimidazoles. 1. Structural features associated with aerobic and anaerobic activities of 4- and 5-nitroimidazoles. | Journal of medicinal chemistry 20090312 |
| Structure-activity relationships of antitubercular nitroimidazoles. 2. Determinants of aerobic activity and quantitative structure-activity relationships. | Journal of medicinal chemistry 20090312 |
| Synthesis, reduction potentials, and antitubercular activity of ring A/B analogues of the bioreductive drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). | Journal of medicinal chemistry 20090212 |
| Microbiology. An antibiotic mimics immunity. | Science (New York, N.Y.) 20081128 |
| PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release. | Science (New York, N.Y.) 20081128 |
| A microbiological assessment of novel nitrofuranylamides as anti-tuberculosis agents. | The Journal of antimicrobial chemotherapy 20081101 |
| Crystal structures of F420-dependent glucose-6-phosphate dehydrogenase FGD1 involved in the activation of the anti-tuberculosis drug candidate PA-824 reveal the basis of coenzyme and substrate binding. | The Journal of biological chemistry 20080620 |
| Intermediates in the reduction of the antituberculosis drug PA-824, (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine, in aqueous solution. | Organic & biomolecular chemistry 20080607 |
| Synthesis and antitubercular activity of 7-(R)- and 7-(S)-methyl-2-nitro-6-(S)-(4-(trifluoromethoxy)benzyloxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazines, analogues of PA-824. | Bioorganic & medicinal chemistry letters 20080401 |
| [Some new antitubercular agents]. | Revue medicale suisse 20080319 |
| PA-824. | Tuberculosis (Edinburgh, Scotland) 20080301 |
| Comparison of the sterilising activities of the nitroimidazopyran PA-824 and moxifloxacin against persisting Mycobacterium tuberculosis. | The international journal of tuberculosis and lung disease : the official journal of the International Union against Tuberculosis and Lung Disease 20080101 |
| New anti-tuberculosis drugs with novel mechanisms of action. | Current medicinal chemistry 20080101 |
| Advances in the treatment of tuberculosis. | Clinical pharmacology and therapeutics 20071101 |
| NLCQ-1 and NLCQ-2, two new agents with activity against dormant Mycobacterium tuberculosis. | International journal of antimicrobial agents 20070601 |
| OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. | PLoS medicine 20061101 |
| Combination chemotherapy with the nitroimidazopyran PA-824 and first-line drugs in a murine model of tuberculosis. | Antimicrobial agents and chemotherapy 20060801 |
| NIAID researchers make key discovery in development of TB drug candidate. | Journal of investigative medicine : the official publication of the American Federation for Clinical Research 20060301 |
| Identification of a nitroimidazo-oxazine-specific protein involved in PA-824 resistance in Mycobacterium tuberculosis. | Proceedings of the National Academy of Sciences of the United States of America 20060110 |
| New tuberculosis drug enters human trials. | The Lancet. Infectious diseases 20050801 |
| New small-molecule synthetic antimycobacterials. | Antimicrobial agents and chemotherapy 20050601 |
| Bactericidal activity of the nitroimidazopyran PA-824 in a murine model of tuberculosis. | Antimicrobial agents and chemotherapy 20050601 |
| Preclinical testing of the nitroimidazopyran PA-824 for activity against Mycobacterium tuberculosis in a series of in vitro and in vivo models. | Antimicrobial agents and chemotherapy 20050601 |
| [Anti-tuberculosis drugs]. | Nihon rinsho. Japanese journal of clinical medicine 20030201 |
| A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. | Nature 20000622 |