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 50 papers

Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units

Publication: Bioorganic & Medicinal Chemistry Letters

Author(s): Peter Choi, Hamish Sutherland, Amy S.T.Tong, Adrian Blaser, Scott Franzblau, Christopher B.Cooper, Manisha U.Lotlikar, Anna M.Upton, Jerome Guillemont, Magali Motte, Laurence Queguiner, Koen Andries, Walter Van den Broeck, William A.Denny, Brian D.Palmer

10/2017

Tags: Bedaquiline (TMC-207), Drug Discovery, M.tb. Biology

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

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

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

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

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