Research Papers

This database includes peer-reviewed publications authored or funded by TB Alliance. Use the tags on the right to filter by subject, or search for a particular author or term using the search bar.

Displaying 132 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)

1/2010 - 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

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data

Toward an Optimized Therapy for Tuberculosis? Drugs in Clinical Trials and in Preclinical Development

12/2009 - Ma Z, Lienhardt C. Toward an optimized therapy for tuberculosis? Drugs in clinical trials and in preclinical development. Clin Chest Med. 2009 Dec;30(4):755-68, ix. doi: 10.1016/j.ccm.2009.08.011.

Tags: Advocacy, Clinical Development, Drug Discovery, Editorials, Global Pipeline, MDR-TB, TB-HIV

Release of nitrite from the antitubercular nitroimidazole drug PA-824 and analogues upon one-electron reduction in protic, non-aqueous solvent

11/2009 - 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.

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

Assessment of global capacity to conduct tuberculosis drug development trials- do we have what it takes

11/2009 - van Niekerk C, Ginsberg A. Assessment of global capacity to conduct tuberculosis drug development trials: do we have what it takes? Int J Tuberc Lung Dis. 2009 Nov;13(11):1367-72. http://www.ingentaconnect.com/content/iuatld/ijtld/2009/00000013/00000011/a

Tags: Advocacy, Clinical Development, Policy

Potent biphenyl- and 3-phenyl pyridine-based inhibitors of acetyl-CoA carboxylase

10/2009 - 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.

Tags: Drug Discovery, Drug Targets, Preclinical Data

Synthesis and Structure-activity Relationships of Antitubercular 2-Nitroimidazooxazines Bearing Heterocyclic Side Chains

9/2009 - 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.

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data

Assessment of the Effects of the Nitroimidazo-Oxazine PA-824 on

6/2009 - Ginsberg AM, Laurenzi MW, Rouse DJ, Whitney KD, Spigelman MK. Assessment of the effects of the nitroimidazo-oxazine PA-824 on renal function in healthy subjects. Antimicrob Agents Chemother. 2009 Sep;53(9):3726-33. doi: 10.1128/AAC.00112-09

Tags: Advocacy, Clinical Development, Clinical Trial Results, Pretomanid/PA-824

Safety, Tolerability, and Pharmacokinetics of PA-824 in Healthy Subjects

6/2009 - Ginsberg AM, Laurenzi MW, Rouse DJ, Whitney KD, Spigelman, MK. Safety, tolerability, and pharmacokinetics of PA-824 in healthy subjects. Antimicrob Agents Chemother. 2009 Sep;53(9):3720-5. doi: 10.1128/AAC.00106-09.

Tags: Clinical Development, Clinical Trial Results, Pharmacodynamics, Pretomanid/PA-824

Acid Resistance in Mycobacterium tuberculosis

5/2009 - Vandal OH, Nathan CF, Ehrt S. Acid resistance in Mycobacterium tuberculosis. J Bacteriol. 2009 Aug;191(15):4714-21. doi: 10.1128/JB.00305-09.

Tags: Advocacy, Drug Discovery, Drug Targets, M.tb. Biology

Dose-ranging comparison of rifampin and rifapentine in two pathologically distinct murine models of tuberculosis

2/2009 - 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

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

2/2009 - 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

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data

Acid-susceptible mutants of Mycobacterium tuberculosis share hypersusceptibility to cell wall and oxidative stress and to the host environment

11/2008 - 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

Tags: Drug Discovery, Drug Targets, M.tb. Biology

Emerging Drugs for Active Tuberculosis

10/2008 - Ginsberg AM. Emerging drugs for active tuberculosis. Semin Respir Crit Care Med. 2008 Oct;29(5):552-9. doi: 10.1055/s-0028-1085706.

Tags: Bedaquiline (TMC-207), Clinical Development, Drug Discovery, Editorials, Global Pipeline, Pretomanid/PA-824, Rifapentine

Estimating the market for tuberculosis drugs in industrialized and developing nations

10/2008 - Schwalbe NR, Wells WA, Geaneotes AP, et. al. Estimating the market for tuberculosis drugs in industrialized and developing nations. Int J Tuberc Lung Dis. 2008 Oct;12(10):1173-81. http://www.ingentaconnect.com/content/iuatld/ijtld/2008/00000012/00000010/a

Tags: Regimen Change, TB Burden, TB Drug Market, TB Market

Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1

5/2008 - 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.

Tags: Drug Discovery, Drug Targets, Preclinical Data

Timing of Default From Tuberculosis Treatment: A Systematic Review

5/2008 - Kruk ME, Schwalbe NR, Aguiar CA. Timing of default from tuberculosis treatment: a systematic review. Trop Med Int Health. 2008 May;13(5):703-12. doi: 10.1111/j.1365-3156.2008.02042.x.

Tags: Advocacy, Policy, Regimen Change, TB Market

The ethics of non-inferiority trials

3/2008 - Nunn AJ, Meredith SK, Spigelman MK, Ginsberg AM, Gillespie SH. The ethics of non-inferiority trials. Lancet. 2008 Mar 15;371(9616):895; author reply 896-7. doi: 10.1016/S0140-6736(08)60404-3.

Tags: Advocacy, Clinical Development, Clinical Trial Results, Editorials, Policy, Trial Design

Handbook of anti-tuberculosis agents

3/2008 - Handbook of Anti-Tuberculosis Agents. Tuberculosis (Edinb). 2008 Mar;88(2):85-6. doi: 10.1016/S1472-9792(08)70002-7.

Tags: Clinical Development, Clofazamine, Global Pipeline, HRZE, Linezolid, Moxifloxacin, Pharmacodynamics, Pharmacokinetics, Pyrazinamide, Rifapentine, Sutezolid

Advancing the science in clinical trials for new TB drugs

2/2008 - Wells WA, Brooks A. Adoption of new health products in low and middle income settings: how product development partnerships can support country decision making. Health Res Policy Syst. 2011 Mar 31;9:15. doi: 10.1186/1478-4505-9-15.

Tags: Biomarkers, Clinical Development, Editorials, Moxifloxacin, Trial Design

New tuberculosis therapeutics: a growing pipeline

8/2007 - Spigelman MK New tuberculosis therapeutics: a growing pipeline. J Infect Dis. 2007 Aug 15;196 Suppl 1:S28-34. http://jid.oxfordjournals.org/content/196/Supplement_1/S28.long. Accessed March 7, 2016

Tags: Clinical Development, Editorials, Global Pipeline, MDR-TB, Moxifloxacin, Pretomanid/PA-824, Rifapentine, TB-HIV

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