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62 results

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Discovery of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator.
Ward SE, Harries M, Aldegheri L, Andreotti D, Ballantine S, Bax BD, Harris AJ, Harker AJ, Lund J, Melarange R, Mingardi A, Mookherjee C, Mosley J, Neve M, Oliosi B, Profeta R, Smith KJ, Smith PW, Spada S, Thewlis KM, Yusaf SP. Ward SE, et al. Among authors: bax bd. J Med Chem. 2010 Aug 12;53(15):5801-12. doi: 10.1021/jm1005429. J Med Chem. 2010. PMID: 20614889 Clinical Trial.
Integration of lead optimization with crystallography for a membrane-bound ion channel target: discovery of a new class of AMPA receptor positive allosteric modulators.
Ward SE, Harries M, Aldegheri L, Austin NE, Ballantine S, Ballini E, Bradley DM, Bax BD, Clarke BP, Harris AJ, Harrison SA, Melarange RA, Mookherjee C, Mosley J, Dal Negro G, Oliosi B, Smith KJ, Thewlis KM, Woollard PM, Yusaf SP. Ward SE, et al. Among authors: bax bd. J Med Chem. 2011 Jan 13;54(1):78-94. doi: 10.1021/jm100679e. Epub 2010 Dec 3. J Med Chem. 2011. PMID: 21128618
Structure-guided design of antibacterials that allosterically inhibit DNA gyrase.
Thalji RK, Raha K, Andreotti D, Checchia A, Cui H, Meneghelli G, Profeta R, Tonelli F, Tommasi S, Bakshi T, Donovan BT, Howells A, Jain S, Nixon C, Quinque G, McCloskey L, Bax BD, Neu M, Chan PF, Stavenger RA. Thalji RK, et al. Among authors: bax bd. Bioorg Med Chem Lett. 2019 Jun 1;29(11):1407-1412. doi: 10.1016/j.bmcl.2019.03.029. Epub 2019 Mar 22. Bioorg Med Chem Lett. 2019. PMID: 30962087
1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.
Christopher JA, Atkinson FL, Bax BD, Brown MJ, Champigny AC, Chuang TT, Jones EJ, Mosley JE, Musgrave JR. Christopher JA, et al. Among authors: bax bd. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2230-4. doi: 10.1016/j.bmcl.2009.02.098. Epub 2009 Feb 28. Bioorg Med Chem Lett. 2009. PMID: 19303774
Identification of 2-(4-pyridyl)thienopyridinones as GSK-3β inhibitors.
Gentile G, Bernasconi G, Pozzan A, Merlo G, Marzorati P, Bamborough P, Bax B, Bridges A, Brough C, Carter P, Cutler G, Neu M, Takada M. Gentile G, et al. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4823-7. doi: 10.1016/j.bmcl.2011.06.050. Epub 2011 Jun 29. Bioorg Med Chem Lett. 2011. PMID: 21764580
5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.
Gentile G, Merlo G, Pozzan A, Bernasconi G, Bax B, Bamborough P, Bridges A, Carter P, Neu M, Yao G, Brough C, Cutler G, Coffin A, Belyanskaya S. Gentile G, et al. Bioorg Med Chem Lett. 2012 Mar 1;22(5):1989-94. doi: 10.1016/j.bmcl.2012.01.034. Epub 2012 Jan 21. Bioorg Med Chem Lett. 2012. PMID: 22310227
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. 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
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. 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
62 results