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 52 papers
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
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
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
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
Structural insight into serine protease Rv3671c that Protects M. tuberculosis from oxidative and acidic stress
Publication: 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.
10/2011
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
Challenges and opportunities in developing novel drugs for TB
Publication: 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.
9/2011
Drugs for neglected diseases: part II
Publication: Kaneko T. Drugs for neglected diseases: part II. Future Med Chem. 2011 Sep;3(11):1329-30. doi: 10.4155/fmc.11.104.
9/2011
Drugs for neglected diseases: part I
Publication: Kaneko T. Drugs for neglected diseases: part I. Future Med Chem. 2011 Aug;3(10):1235-7. doi: 10.4155/fmc.11.103.
8/2011
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
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
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
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
Current development and future prospects in chemotherapy of tuberculosis
Publication: Nuermberger EL, Spigelman MK, Yew WW. Current development and future prospects in chemotherapy of tuberculosis. Respirology. 2010 Jul;15(5):764-78. doi: 10.1111/j.1440-1843.2010.01775.x.
7/2010
Development of a population pharmacokinetic model for taranabant, a cannibinoid-1 receptor inverse agonist
Publication: Li X (Susie), Nielsen J, Cirincione B, et. al. Development of a Population Pharmacokinetic Model for Taranabant, a Cannibinoid-1 Receptor Inverse Agonist. The AAPS Journal. 2010;12(4):537-547. doi:10.1208/s12248-010-9212-2.
6/2010
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)
Publication: 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
1/2010
Toward an Optimized Therapy for Tuberculosis? Drugs in Clinical Trials and in Preclinical Development
Publication: 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.
12/2009
Release of nitrite from the antitubercular nitroimidazole drug PA-824 and analogues upon one-electron reduction in protic, non-aqueous solvent
Publication: 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.
11/2009
Potent biphenyl- and 3-phenyl pyridine-based inhibitors of acetyl-CoA carboxylase
Publication: 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.
10/2009
Synthesis and Structure-activity Relationships of Antitubercular 2-Nitroimidazooxazines Bearing Heterocyclic Side Chains
Publication: 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.
9/2009