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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: pearson nd. 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
Exploration of the P1 residue in 3CL protease inhibitors leading to the discovery of a 2-tetrahydrofuran P1 replacement.
Barton LS, Callahan JF, Cantizani J, Concha NO, Cotillo Torrejon I, Goodwin NC, Joshi-Pangu A, Kiesow TJ, McAtee JJ, Mellinger M, Nixon CJ, Padrón-Barthe L, Patterson JR, Pearson ND, Pouliot JJ, Rendina AR, Buitrago Santanilla A, Schneck JL, Sanz O, Thalji RK, Ward P, Williams SP, King BW. Barton LS, et al. Among authors: pearson nd. Bioorg Med Chem. 2024 Feb 15;100:117618. doi: 10.1016/j.bmc.2024.117618. Epub 2024 Jan 29. Bioorg Med Chem. 2024. PMID: 38309201
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: pearson nd. Nature. 2010 Aug 19;466(7309):935-40. doi: 10.1038/nature09197. Epub 2010 Aug 4. Nature. 2010. PMID: 20686482
RNA as a drug target.
Pearson ND, Prescott CD. Pearson ND, et al. Chem Biol. 1997 Jun;4(6):409-14. doi: 10.1016/s1074-5521(97)90192-7. Chem Biol. 1997. PMID: 9224569
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: pearson nd. 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
12 results