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 28 papers

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

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data

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

Tags: Drug Discovery, Preclinical Data, Pretomanid/PA-824

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

Tags: Drug Discovery, Drug Targets, Preclinical Data

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

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data

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

Tags: Drug Discovery, Editorials, Global Pipeline, HRZE, Preclinical Data, Preclinical Models, Pyrazinamide, Rifapentine

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

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data

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

Tags: Drug Discovery, Drug Targets, Preclinical Data

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

Tags: Drug Discovery, Drug Targets, M.tb. Biology, MDR-TB, Preclinical Data

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