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: Drug Discovery

Displaying 49 papers

Tuberculosis

Publication: Tuberculosis.Nature Reviews Disease Primers. 2016/10/27/online. 16076. Macmillan Publishers Limited. http://dx.doi.org/10.1038/nrdp.2016.76

Author(s): Pai, Madhukar; Behr, Marcel A.; Dowdy, David; Dheda, Keertan; Divangahi, Maziar; Boehme, Catharina C.; Ginsberg, Ann; Swaminathan, Soumya; Spigelman, Melvin; Getahun, Haileyesus; Menzies, Dick; Raviglione, Mario

10/2016

Tags: Clinical Development, Drug Discovery, MDR-TB, TB-HIV

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

The Tuberculosis Drug Discovery and Development Pipeline and Emerging Drug Targets

Publication: Mdluli K, Kaneko T, Upton A. The tuberculosis drug discovery and development pipeline and emerging drug targets.Cold Spring Harb Perspect Med. 2015 Jan 29;5(6). pii: a021154. doi: 10.1101/cshperspect.a021154.

1/2015

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

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

Lead optimization of 1,4-azaindoles as antimycobacterial agents

Publication: Shirude PS, Shandil RK, Manjunatha MR, et. al. Lead optimization of 1,4-azaindoles as antimycobacterial agents. J Med Chem. 2014 Jul 10;57(13):5728-37. doi: 10.1021/jm500571f.

6/2014

Tags: Drug Discovery, Pharmacokinetics

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

Tuberculosis drug discovery and emerging targets

Publication: Mdluli K, Kaneko T, Upton A. Tuberculosis drug discovery and emerging targets. Ann N Y Acad Sci. 2014 Sep;1323:56-75. doi: 10.1111/nyas.12459.

6/2014

Tags: Advocacy, Drug Discovery, Drug Targets, Editorials, Preclinical Models

Development of Mycobacterium tuberculosis whole cell screening hits as potential antituberculosis agents

Publication: Cooper CB. Development of Mycobacterium tuberculosis whole cell screening hits as potential antituberculosis agents. J Med Chem. 2013 Oct 24;56(20):7755-60. doi: 10.1021/jm400381v.

10/2013

Tags: Drug Discovery, Global Pipeline, Preclinical Models

Identification of a small molecule with activity against drug-resistant and persistent tuberculosis

Publication: Wang F, Sambandan D, Halder R, et. al. Identification of a small molecule with activity against drug-resistant and persistent tuberculosis. Proc Natl Acad Sci U S A. 2013 Jul 2;110(27):E2510-7. doi: 10.1073/pnas.1309171110.

5/2013

Tags: Drug Discovery, Drug Targets, MDR-TB, Preclinical Models

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

Reply to "Contradictory results with high-dosage rifamycin in mice and humans"

Publication: Nuermberger EL, Rosenthal IM, Tasneen R, et. al. Reply to "Contradictory results with high-dosage rifamycin in mice and humans". Antimicrob Agents Chemother. 2013 Feb;57(2):1104-5. doi: 10.1128/AAC.02216-12

2/2013

Tags: Drug Discovery, Editorials, Pharmacodynamics, Preclinical Models, Rifapentine

Comprehensive analysis of methods used for the evaluation of compounds against Mycobacterium tuberculosis

Publication: Franzblau SG, DeGroote MA, Cho SH, et. al. Comprehensive analysis of methods used for the evaluation of compounds against Mycobacterium tuberculosis. Tuberculosis (Edinb). 2012 Nov;92(6):453-88. doi: 10.1016/j.tube.2012.07.003.

11/2012

Tags: Advocacy, Drug Discovery, Editorials, Preclinical Models

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

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

Publication: 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.

3/2012

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

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

Publication: 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.

3/2012

Tags: Advocacy, Drug Discovery, Drug Targets, Editorials

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

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)

Publication: 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

12/2011

Tags: Drug Discovery, Pharmacodynamics

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