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

Identification of Less Lipophilic Riminophenazine Derivatives for the Treatment of Drug-Resistant Tuberculosis

9/2012 - Zhang D, Lu Y, Liu K, et. al. Identification of less lipophilic riminophenazine derivatives for the treatment of drug-resistant tuberculosis. J Med Chem. 2012 Oct 11;55(19):8409-17. doi: 10.1021/jm300828h.

Tags: Clofazamine, Drug Discovery, MDR-TB, Preclinical Data

Diphenylpyridylethanamine (DPPE) derivatives as cholesteryl ester transfer protein (CETP) inhibitors

7/2012 - Harikrishnan LS, Finlay HJ, Qiao JX, Kamau MG, et. al. Diphenylpyridylethanamine (DPPE) derivatives as cholesteryl ester transfer protein (CETP) inhibitors. J Med Chem. 2012 Jul 12;55(13):6162-75. doi: 10.1021/jm300611v.

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data

In vitro and in vivo activity of clofazimine against Mycobacterium tuberculosis persisters

6/2012 - Upton AM, Cho S, Yang TJ, et. al. In vitro and in vivo activities of the nitroimidazole TBA-354 against Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2015 Jan;59(1):136-44. doi: 10.1128/AAC.03823-14.

Tags: Clofazamine, Drug Discovery, Moxifloxacin, Preclinical Data

Rifapentine is not more active than rifampin against chronic tuberculosis in guinea pigs

4/2012 - Dutta NK, Illei PB, Peloquin CA, et. al. Rifapentine Is Not More Active than Rifampin against Chronic Tuberculosis in Guinea Pigs. http://aac.asm.org/content/56/7/3726.long. Accessed March 7, 2016

Tags: Preclinical Data, Rifapentine

Systematic Evaluation of Structure-Activity Relationships of the Riminophenazine Class and Discovery of a C2 Pyridylamino Series for the Treatment of Multidrug-Resistant Tuberculosis

4/2012 - Liu B, Liu K, Yang TJ, et. al. Systematic evaluation of structure-activity relationships of... Molecules. 2012 Apr 17;17(4):4545-59. doi: 10.3390/molecules17044545.

Tags: Clofazamine, Drug Discovery, Pharmacokinetics, Preclinical Data

Sterilizing Activities of Novel Combinations Lacking First- and Second-Line Drugs in a Murine Model of Tuberculosis

4/2012 - Williams K, Minkowski A, Amoabeng O, et. al. Sterilizing activities of novel combinations lacking first- and second-line drugs in a murine model of tuberculosis. Antimicrob Agents Chemother. 2012 Jun;56(6):3114-20. doi: 10.1128/AAC.00384-12.

Tags: Bedaquiline (TMC-207), Clofazamine, Preclinical Data, Pretomanid/PA-824, Pyrazinamide, Rifapentine, Sutezolid

Strategies and challenges involved in the discovery of new chemical entities during early-stage tuberculosis drug discovery

3/2012 - Coxon GD, Cooper CB, Gillespie SH, McHugh TD. Strategies and challenges involved in the discovery of new chemical entities during early-stage tuberculosis drug discovery. J Infect Dis. 2012 May 15;205 Suppl 2:S258-64. doi: 10.1093/infdis/jis191.

Tags: Advocacy, Drug Discovery, Drug Targets, Editorials

Phase II dose-ranging trial of the early bactericidal activity of PA-824

3/2012 - Diacon AH, Dawson R, du Bois J, et. al. Phase II dose-ranging trial of the early bactericidal activity of PA-824. Antimicrob Agents Chemother. 2012 Jun;56(6):3027-31. doi: 10.1128/AAC.06125-11

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

Moxifloxacin for tuberculosis

3/2012 - Mendel C, Springsklee M. Moxifloxacin for tuberculosis. Lancet Infect Dis. 2012 Mar;12(3):176-7; author reply 177-8. doi: 10.1016/S1473-3099(11)70351-6.

Tags: Advocacy, Clinical Development, Drug-Sensitivity Testing, Editorials, MDR-TB, Moxifloxacin, Policy, Regimen Change

New Drugs for the Treatment of Tuberculosis: Needs, Challenges, Promise, and Prospects for the Future

3/2012 - Lienhardt C, Raviglione M, Spigelman M, et. al. New drugs for the treatment of tuberculosis: needs, challenges, promise, and prospects for the future. J Infect Dis. 2012 May 15;205 Suppl 2:S241-9. doi: 10.1093/infdis/jis034.

Tags: Advocacy, Childhood TB, Clinical Development, Drug Discovery, Drug-Sensitivity Testing, Editorials, Global Pipeline, MDR-TB, Moxifloxacin, Pharmacodynamics, Pharmacokinetics, Policy, Preclinical Models, Pretomanid/PA-824, Regimen Change, TB Market, TB-HIV, Trial Design

Identification and optimization of small molecule antagonists of vasoactive intestinal peptide receptor-1 (VIPR1)

2/2012 - Harikrishnan LS, Srivastava N, Kayser LE, et. al. Identification and optimization of small molecule antagonists of vasoactive intestinal peptide receptor-1 (VIPR1). Bioorg Med Chem Lett. 2012 Mar 15;22(6):2287-90. doi: 10.1016/j.bmcl.2012.01.082.

Tags: Drug Discovery, Preclinical Data

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)

12/2011 - Blaser A, Palmer BD, Sutherland HS, et. al. 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). J

Tags: Drug Discovery, Pharmacodynamics

Clofazimine Analogs with Efficacy against Experimental Tuberculosis and Reduced Potential for Accumulation

11/2011 - Yu Lu, Meiqin Zheng, Bin Wang, et. al. Clofazimine Analogs with Efficacy against Experimental Tuberculosis and Reduced Potential for Accumulation. Antimicrob Agents Chemother. 2011 Nov; 55(11): 5185–5193. doi: 10.1128/AAC.00699-11

Tags: Clofazamine, Drug Discovery, Preclinical Data

Structural insight into serine protease Rv3671c that Protects M. tuberculosis from oxidative and acidic stress

10/2011 - Biswas T, Small J, Vandal O, et. al. Structural insight into serine protease Rv3671c that protects M. tuberculosis from oxidative and acidic stress. Structure. 2010 Oct 13;18(10):1353-63. doi: 10.1016/j.str.2010.06.017.

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

Sterilizing activity of novel TMC207- and PA-824-containing regimens in a murine model of tuberculosis

9/2011 - Tasneen R, Li SY, Peloquin CA, et. al. Sterilizing activity of novel TMC207- and PA-824-containing regimens in a murine model of tuberculosis. Antimicrob Agents Chemother. 2011 Dec;55(12):5485-92. doi: 10.1128/AAC.05293-11

Tags: Bedaquiline (TMC-207), BPaZ, Clofazamine, Preclinical Data, Pretomanid/PA-824

Synthesis and Structure-activity Relationships of Varied Ether Linker Analogues of the Anti-tubercular Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (

9/2011 - Thompson AM, Sutherland HS, Palmer BD, et. al. 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).

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data

14-day bactericidal activity of PA-824, bedaquiline, pyrazinamide, and moxifloxacin combinations: a randomised trial.

9/2011 - Diacon AH, Dawson R, von Groote-Bidlingmaier F, et. al. 14-day bactericidal activity of PA-824, bedaquiline, pyrazinamide, and moxifloxacin combinations: a randomised trial. Lancet. 2012 Sep 15;380(9846):986-93. doi: 10.1016/S0140-6736(12)61080-0.

Tags: Bedaquiline (TMC-207), Clinical Development, Clinical Trial Results, MDR-TB, Moxifloxacin, NC-001, PaMZ, Pretomanid/PA-824, Pyrazinamide

Challenges and opportunities in developing novel drugs for TB

9/2011 - Kaneko T, Cooper C, Mdluli K. Challenges and opportunities in developing novel drugs for TB. Future Med Chem. 2011 Sep;3(11):1373-400. doi: 10.4155/fmc.11.115.

Author(s): Takushi Kaneko, Christopher Cooper, Khisimuzi Mdluli

Tags: Advocacy, Drug Discovery, Editorials, Global Pipeline, Preclinical Models

Drugs for neglected diseases: part II

9/2011 - Kaneko T. Drugs for neglected diseases: part II. Future Med Chem. 2011 Sep;3(11):1329-30. doi: 10.4155/fmc.11.104.

Tags: Advocacy, Clinical Development, Drug Discovery, Editorials, Global Pipeline, TB Burden

Drug repositioning in the treatment of malaria and TB

9/2011 - Nzila A, Ma Z, Chibale K. Drug repositioning in the treatment of malaria and TB. Future Med Chem. 2011 Sep;3(11):1413-26. doi: 10.4155/fmc.11.95.

Author(s): Alexis Nzil, Zhenkun Ma, Kelly Chibale

Tags: Advocacy, Editorials, MDR-TB, TB Burden, XDR-TB

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