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

Evaluation of moxifloxacin-containing regimens in pathologically distinct murine tuberculosis models

Publication: Li SY, Irwin SM, Converse PJ, Mdluli KE, Lenaerts AJ, Nuermberger EL. Evaluation of moxifloxacin-containing regimens in pathologically distinct murine tuberculosis models. Antimicrob Agents Chemother. 2015 Jul;59(7):4026-30. doi: 10.1128/AAC.00105-15.

4/2015

Tags: Clinical Development, HRZE, Moxifloxacin, Preclinical Data, Preclinical Models, ReMoxTB

Contribution of the Nitroimidazoles PA-824 and TBA-354 to the Activity of Novel Regimens in Murine Models of Tuberculosis

Publication: Tasneen R, Williams K, Amoabeng O, Minkowski A, Mdluli KE, Upton AM, Nuermberger EL. Contribution of the nitroimidazoles PA-824 and TBA-354 to the activity of novel regimens in murine models of tuberculosis. Antimicrob Agents Chemother. 2015 Jan;59(1):129

1/2015

Tags: Drug Discovery, Linezolid, Preclinical Data, Pretomanid/PA-824, Pyrazinamide, Sutezolid, TBA-354

In Vitro and In Vivo Activities of the Nitroimidazole TBA-354 against Mycobacterium tuberculosis

Publication: 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.

10/2014

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data, TBA-354

1,4-Azaindole, a Potential Drug Candidate for Treatment of Tuberculosis

Publication: Chatterji M, Shandil R, Manjunatha MR, et. al. 1,4-azaindole, a potential drug candidate for treatment of tuberculosis.Antimicrob Agents Chemother. 2014 Sep;58(9):5325-31. doi: 10.1128/AAC.03233-14.

6/2014

Tags: Bedaquiline (TMC-207), Drug Discovery, MDR-TB, Pharmacokinetics, Preclinical Data, Pretomanid/PA-824

Potent rifamycin-sparing regimen cures guinea pig tuberculosis as rapidly as the standard regimen

Publication: Dutta NK, Alsultan A, Gniadek TJ, et. al. Potent rifamycin-sparing regimen cures guinea pig tuberculosis as rapidly as the standard regimen. Antimicrob Agents Chemother. 2013 Aug;57(8):3910-6. doi: 10.1128/AAC.00761-13.

8/2013

Tags: HRZE, Moxifloxacin, PaMZ, Preclinical Data, Pretomanid/PA-824, Pyrazinamide

Design, synthesis, and structure-activity relationship studies of tryptanthrins as antitubercular agents

Publication: Hwang JM, Oh T, Kaneko T., et. al. Design, synthesis, and structure-activity relationship studies of tryptanthrins as antitubercular agents. J Nat Prod. 2013 Mar 22;76(3):354-67. doi: 10.1021/np3007167.

3/2013

Tags: Drug Discovery, Pharmacodynamics, Pharmacokinetics, Preclinical Data

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

Publication: 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.

9/2012

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

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

Publication: 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.

7/2012

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data

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

Publication: 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.

6/2012

Tags: Clofazamine, Drug Discovery, Moxifloxacin, Preclinical Data

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

Publication: 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.

4/2012

Tags: Clofazamine, Drug Discovery, Pharmacokinetics, Preclinical Data

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

Publication: 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.

4/2012

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

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

Publication: 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

4/2012

Tags: Preclinical Data, Rifapentine

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

Publication: 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.

2/2012

Tags: Drug Discovery, Preclinical Data

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

Publication: 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

11/2011

Tags: Clofazamine, Drug Discovery, Preclinical Data

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 (

Publication: 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).

9/2011

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data

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

Publication: 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

9/2011

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

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

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data, XDR-TB

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

Tags: Drug Discovery, Preclinical Data

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

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data

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

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

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