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Page 1
Structure-activity relationships of antitubercular nitroimidazoles. 3. Exploration of the linker and lipophilic tail of ((s)-2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazin-6-yl)-(4-trifluoromethoxybenzyl)amine (6-amino PA-824).
Cherian J, Choi I, Nayyar A, Manjunatha UH, Mukherjee T, Lee YS, Boshoff HI, Singh R, Ha YH, Goodwin M, Lakshminarayana SB, Niyomrattanakit P, Jiricek J, Ravindran S, Dick T, Keller TH, Dartois V, Barry CE 3rd. Cherian J, et al. Among authors: keller th. J Med Chem. 2011 Aug 25;54(16):5639-59. doi: 10.1021/jm1010644. Epub 2011 Jul 26. J Med Chem. 2011. PMID: 21755942 Free PMC article.
Synthesis and antitubercular activity of 7-(R)- and 7-(S)-methyl-2-nitro-6-(S)-(4-(trifluoromethoxy)benzyloxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazines, analogues of PA-824.
Li X, Manjunatha UH, Goodwin MB, Knox JE, Lipinski CA, Keller TH, Barry CE 3rd, Dowd CS. Li X, et al. Among authors: keller th. Bioorg Med Chem Lett. 2008 Apr 1;18(7):2256-62. doi: 10.1016/j.bmcl.2008.03.011. Epub 2008 Mar 7. Bioorg Med Chem Lett. 2008. PMID: 18358721 Free PMC article.
Structure-activity relationships of antitubercular nitroimidazoles. 2. Determinants of aerobic activity and quantitative structure-activity relationships.
Kim P, Kang S, Boshoff HI, Jiricek J, Collins M, Singh R, Manjunatha UH, Niyomrattanakit P, Zhang L, Goodwin M, Dick T, Keller TH, Dowd CS, Barry CE 3rd. Kim P, et al. Among authors: keller th. J Med Chem. 2009 Mar 12;52(5):1329-44. doi: 10.1021/jm801374t. J Med Chem. 2009. PMID: 19209893 Free PMC article.
PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release.
Singh R, Manjunatha U, Boshoff HI, Ha YH, Niyomrattanakit P, Ledwidge R, Dowd CS, Lee IY, Kim P, Zhang L, Kang S, Keller TH, Jiricek J, Barry CE 3rd. Singh R, et al. Among authors: keller th. Science. 2008 Nov 28;322(5906):1392-5. doi: 10.1126/science.1164571. Science. 2008. PMID: 19039139 Free PMC article.
Spirotetrahydro beta-carbolines (spiroindolones): a new class of potent and orally efficacious compounds for the treatment of malaria.
Yeung BK, Zou B, Rottmann M, Lakshminarayana SB, Ang SH, Leong SY, Tan J, Wong J, Keller-Maerki S, Fischli C, Goh A, Schmitt EK, Krastel P, Francotte E, Kuhen K, Plouffe D, Henson K, Wagner T, Winzeler EA, Petersen F, Brun R, Dartois V, Diagana TT, Keller TH. Yeung BK, et al. Among authors: keller maerki s, keller th. J Med Chem. 2010 Jul 22;53(14):5155-64. doi: 10.1021/jm100410f. J Med Chem. 2010. PMID: 20568778 Free PMC article.
A chemical genetic screen in Mycobacterium tuberculosis identifies carbon-source-dependent growth inhibitors devoid of in vivo efficacy.
Pethe K, Sequeira PC, Agarwalla S, Rhee K, Kuhen K, Phong WY, Patel V, Beer D, Walker JR, Duraiswamy J, Jiricek J, Keller TH, Chatterjee A, Tan MP, Ujjini M, Rao SP, Camacho L, Bifani P, Mak PA, Ma I, Barnes SW, Chen Z, Plouffe D, Thayalan P, Ng SH, Au M, Lee BH, Tan BH, Ravindran S, Nanjundappa M, Lin X, Goh A, Lakshminarayana SB, Shoen C, Cynamon M, Kreiswirth B, Dartois V, Peters EC, Glynne R, Brenner S, Dick T. Pethe K, et al. Among authors: keller th. Nat Commun. 2010 Aug 24;1(5):57. doi: 10.1038/ncomms1060. Nat Commun. 2010. PMID: 20975714 Free PMC article.
Peptide deformylase inhibitors of Mycobacterium tuberculosis: synthesis, structural investigations, and biological results.
Pichota A, Duraiswamy J, Yin Z, Keller TH, Alam J, Liung S, Lee G, Ding M, Wang G, Chan WL, Schreiber M, Ma I, Beer D, Ngew X, Mukherjee K, Nanjundappa M, Teo JW, Thayalan P, Yap A, Dick T, Meng W, Xu M, Koehn J, Pan SH, Clark K, Xie X, Shoen C, Cynamon M. Pichota A, et al. Among authors: keller th. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6568-72. doi: 10.1016/j.bmcl.2008.10.040. Epub 2008 Oct 14. Bioorg Med Chem Lett. 2008. PMID: 19008098
N-sulfonylanthranilic acid derivatives as allosteric inhibitors of dengue viral RNA-dependent RNA polymerase.
Yin Z, Chen YL, Kondreddi RR, Chan WL, Wang G, Ng RH, Lim JY, Lee WY, Jeyaraj DA, Niyomrattanakit P, Wen D, Chao A, Glickman JF, Voshol H, Mueller D, Spanka C, Dressler S, Nilar S, Vasudevan SG, Shi PY, Keller TH. Yin Z, et al. Among authors: keller th. J Med Chem. 2009 Dec 24;52(24):7934-7. doi: 10.1021/jm901044z. J Med Chem. 2009. PMID: 20014868
96 results