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Page 1
Easy-To-Synthesize Spirocyclic Compounds Possess Remarkable in Vivo Activity against Mycobacterium tuberculosis.
Guardia A, Baiget J, Cacho M, Pérez A, Ortega-Guerra M, Nxumalo W, Khanye SD, Rullas J, Ortega F, Jiménez E, Pérez-Herrán E, Fraile-Gabaldón MT, Esquivias J, Fernández R, Porras-De Francisco E, Encinas L, Alonso M, Giordano I, Rivero C, Miguel-Siles J, Osende JG, Badiola KA, Rutledge PJ, Todd MH, Remuiñán M, Alemparte C. Guardia A, et al. Among authors: giordano i. J Med Chem. 2018 Dec 27;61(24):11327-11340. doi: 10.1021/acs.jmedchem.8b01533. Epub 2018 Dec 12. J Med Chem. 2018. PMID: 30457865
Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)-ol (GSK656).
Li X, Hernandez V, Rock FL, Choi W, Mak YSL, Mohan M, Mao W, Zhou Y, Easom EE, Plattner JJ, Zou W, Pérez-Herrán E, Giordano I, Mendoza-Losana A, Alemparte C, Rullas J, Angulo-Barturen I, Crouch S, Ortega F, Barros D, Alley MRK. Li X, et al. Among authors: giordano i. J Med Chem. 2017 Oct 12;60(19):8011-8026. doi: 10.1021/acs.jmedchem.7b00631. Epub 2017 Sep 27. J Med Chem. 2017. PMID: 28953378
Novel tricyclics (e.g., GSK945237) as potent inhibitors of bacterial type IIA topoisomerases.
Miles TJ, Hennessy AJ, Bax B, Brooks G, Brown BS, Brown P, Cailleau N, Chen D, Dabbs S, Davies DT, Esken JM, Giordano I, Hoover JL, Jones GE, Kusalakumari Sukmar SK, Markwell RE, Minthorn EA, Rittenhouse S, Gwynn MN, Pearson ND. Miles TJ, et al. Among authors: giordano i. Bioorg Med Chem Lett. 2016 May 15;26(10):2464-2469. doi: 10.1016/j.bmcl.2016.03.106. Epub 2016 Mar 31. Bioorg Med Chem Lett. 2016. PMID: 27055939
Novel cyclohexyl-amides as potent antibacterials targeting bacterial type IIA topoisomerases.
Miles TJ, Barfoot C, Brooks G, Brown P, Chen D, Dabbs S, Davies DT, Downie DL, Eyrisch S, Giordano I, Gwynn MN, Hennessy A, Hoover J, Huang J, Jones G, Markwell R, Rittenhouse S, Xiang H, Pearson N. Miles TJ, et al. Among authors: giordano i. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7483-8. doi: 10.1016/j.bmcl.2011.09.114. Epub 2011 Oct 10. Bioorg Med Chem Lett. 2011. PMID: 22030032
Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.
Miles TJ, Axten JM, Barfoot C, Brooks G, Brown P, Chen D, Dabbs S, Davies DT, Downie DL, Eyrisch S, Gallagher T, Giordano I, Gwynn MN, Hennessy A, Hoover J, Huang J, Jones G, Markwell R, Miller WH, Minthorn EA, Rittenhouse S, Seefeld M, Pearson N. Miles TJ, et al. Among authors: giordano i. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7489-95. doi: 10.1016/j.bmcl.2011.09.117. Epub 2011 Oct 10. Bioorg Med Chem Lett. 2011. PMID: 22047689
Novel hydroxyl tricyclics (e.g., GSK966587) as potent inhibitors of bacterial type IIA topoisomerases.
Miles TJ, Hennessy AJ, Bax B, Brooks G, Brown BS, Brown P, Cailleau N, Chen D, Dabbs S, Davies DT, Esken JM, Giordano I, Hoover JL, Huang J, Jones GE, Sukmar SK, Spitzfaden C, Markwell RE, Minthorn EA, Rittenhouse S, Gwynn MN, Pearson ND. Miles TJ, et al. Among authors: giordano i. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5437-41. doi: 10.1016/j.bmcl.2013.07.013. Epub 2013 Jul 17. Bioorg Med Chem Lett. 2013. PMID: 23968823
N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: indazoles as phenol isosteres with improved pharmacokinetics.
Bamborough P, Angell RM, Bhamra I, Brown D, Bull J, Christopher JA, Cooper AW, Fazal LH, Giordano I, Hind L, Patel VK, Ranshaw LE, Sims MJ, Skone PA, Smith KJ, Vickerstaff E, Washington M. Bamborough P, et al. Among authors: giordano i. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4363-8. doi: 10.1016/j.bmcl.2007.04.029. Epub 2007 Apr 13. Bioorg Med Chem Lett. 2007. PMID: 17600705
Type IIA topoisomerase inhibition by a new class of antibacterial agents.
Bax BD, Chan PF, Eggleston DS, Fosberry A, Gentry DR, Gorrec F, Giordano I, Hann MM, Hennessy A, Hibbs M, Huang J, Jones E, Jones J, Brown KK, Lewis CJ, May EW, Saunders MR, Singh O, Spitzfaden CE, Shen C, Shillings A, Theobald AJ, Wohlkonig A, Pearson ND, Gwynn MN. Bax BD, et al. Among authors: giordano i. Nature. 2010 Aug 19;466(7309):935-40. doi: 10.1038/nature09197. Epub 2010 Aug 4. Nature. 2010. PMID: 20686482
56 results