Research Papers
This database includes peer-reviewed publications authored by TB Alliance staff. Use the tags on the left to filter by subject, or search for a particular author or term using the search bar.
Tag: Preclinical Data
Displaying 32 papers
Activity of the Fluoroquinolone DC-159a in the Initial and Continuation Phases of Treatment of Murine Tuberculosis
Publication: Vandal OH, Roberts JA, Odaira T, Schnappinger D, Nathan CF, Ehrt S. Acid-susceptible mutants of Mycobacterium tuberculosis share hypersusceptibility to cell wall and oxidative stress and to the host environment. J Bacteriol. 2009 Jan;191(2):625-31. doi: 1
4/2011
Synthesis and structure-activity relationships of aza- and diazabiphenyl 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)
Publication: Kmentova I, Sutherland HS, Palmer BD, et. al. Synthesis and structure-activity relationships of aza- and diazabiphenyl 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)
11/2010
Analysis and hit filtering of a very large library of compounds screened against Mycobacterium tuberculosis
Publication: Ekins S, Kaneko T, Lipinski CA, et. al. Analysis and hit filtering of a very large library of compounds screened against Mycobacterium tuberculosis. Mol Biosyst. 2010 Nov;6(11):2316-24. doi: 10.1039/c0mb00104j.
11/2010
PA-824 exhibits time-dependent activity in a murine model of tuberculosis
Publication: Ahmad Z, Peloquin CA, Singh RP, et. al. PA-824 exhibits time-dependent activity in a murine model of tuberculosis. Antimicrob Agents Chemother. 2011 Jan;55(1):239-45. doi: 10.1128/AAC.00849-10.
10/2010
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)
Publication: Palmer BD, Thompson AM, Sutherland HS, et. al. 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). J Med Chem. 2010 Ja
1/2010
Release of nitrite from the antitubercular nitroimidazole drug PA-824 and analogues upon one-electron reduction in protic, non-aqueous solvent
Publication: Maroz A, Shinde SS, Franzblau SG, et. al. Release of nitrite from the antitubercular nitroimidazole drug PA-824 and analogues upon one-electron reduction in protic, non-aqueous solvent. Org Biomol Chem. 2010 Jan 21;8(2):413-8. doi: 10.1039/b915877d.
11/2009
Potent biphenyl- and 3-phenyl pyridine-based inhibitors of acetyl-CoA carboxylase
Publication: Haque TS, Liang N, Golla R, et. al. Potent biphenyl- and 3-phenyl pyridine-based inhibitors of acetyl-CoA carboxylase. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5872-6. doi: 10.1016/j.bmcl.2009.08.077.
10/2009
Synthesis and Structure-activity Relationships of Antitubercular 2-Nitroimidazooxazines Bearing Heterocyclic Side Chains
Publication: Sutherland HS, Blaser A, Kmentova I, et. al. Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains. J Med Chem. 2010 Jan 28;53(2):855-66. doi: 10.1021/jm901378u.
9/2009
Dose-ranging comparison of rifampin and rifapentine in two pathologically distinct murine models of tuberculosis
Publication: Rosenthal IM, Tasneen R, Peloquin CA, et. al. Dose-Ranging Comparison of Rifampin and Rifapentine in Two Pathologically Distinct Murine Models of Tuberculosis. Antimicrob Agents Chemother. 2012 Aug; 56(8): 4331–4340. doi: 10.1128/AAC.00912-12
2/2009
Synthesis, Reduction Potentials, and Antitubercular Activity of Ring A/B Analogues of the Bioreductive Drug PA-824
Publication: Thompson AM, Blaser A, Anderson RF, et. al. 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). J
2/2009
Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
Publication: Wang H, Ruan Z, Li JJ, et. al. Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3168-72. doi: 10.1016/j.bmcl.2008.
5/2008
Mycobacterium tuberculosis DNA gyrase as a target for drug discovery
Publication: Mdluli K, Ma Z. Mycobacterium tuberculosis DNA gyrase as a target for drug discovery. Infect Disord Drug Targets. 2007 Jun;7(2):159-68. http://www.ingentaconnect.com/content/ben/iddt/2007/00000007/00000002/art00008?token=00521b85a26b1174e1f7b76504c48662a2
6/2007