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Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice.
Gujjar R, El Mazouni F, White KL, White J, Creason S, Shackleford DM, Deng X, Charman WN, Bathurst I, Burrows J, Floyd DM, Matthews D, Buckner FS, Charman SA, Phillips MA, Rathod PK. Gujjar R, et al. Among authors: creason s. J Med Chem. 2011 Jun 9;54(11):3935-49. doi: 10.1021/jm200265b. Epub 2011 May 12. J Med Chem. 2011. PMID: 21517059 Free PMC article.
Bioisosteric transformations and permutations in the triazolopyrimidine scaffold to identify the minimum pharmacophore required for inhibitory activity against Plasmodium falciparum dihydroorotate dehydrogenase.
Marwaha A, White J, El Mazouni F, Creason SA, Kokkonda S, Buckner FS, Charman SA, Phillips MA, Rathod PK. Marwaha A, et al. Among authors: creason sa. J Med Chem. 2012 Sep 13;55(17):7425-36. doi: 10.1021/jm300351w. Epub 2012 Aug 21. J Med Chem. 2012. PMID: 22877245 Free PMC article.
Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis.
Tatipaka HB, Gillespie JR, Chatterjee AK, Norcross NR, Hulverson MA, Ranade RM, Nagendar P, Creason SA, McQueen J, Duster NA, Nagle A, Supek F, Molteni V, Wenzler T, Brun R, Glynne R, Buckner FS, Gelb MH. Tatipaka HB, et al. Among authors: creason sa. J Med Chem. 2014 Feb 13;57(3):828-35. doi: 10.1021/jm401178t. Epub 2014 Jan 15. J Med Chem. 2014. PMID: 24354316 Free PMC article.
Structure-guided design of novel Trypanosoma brucei Methionyl-tRNA synthetase inhibitors.
Huang W, Zhang Z, Barros-Álvarez X, Koh CY, Ranade RM, Gillespie JR, Creason SA, Shibata S, Verlinde CLMJ, Hol WGJ, Buckner FS, Fan E. Huang W, et al. Among authors: creason sa. Eur J Med Chem. 2016 Nov 29;124:1081-1092. doi: 10.1016/j.ejmech.2016.10.024. Epub 2016 Oct 14. Eur J Med Chem. 2016. PMID: 27788467 Free PMC article.
Optimization of a binding fragment targeting the "enlarged methionine pocket" leads to potent Trypanosoma brucei methionyl-tRNA synthetase inhibitors.
Huang W, Zhang Z, Ranade RM, Gillespie JR, Barros-Álvarez X, Creason SA, Shibata S, Verlinde CLMJ, Hol WGJ, Buckner FS, Fan E. Huang W, et al. Among authors: creason sa. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2702-2707. doi: 10.1016/j.bmcl.2017.04.048. Epub 2017 Apr 17. Bioorg Med Chem Lett. 2017. PMID: 28465105 Free PMC article.
Development of Methionyl-tRNA Synthetase Inhibitors as Antibiotics for Gram-Positive Bacterial Infections.
Faghih O, Zhang Z, Ranade RM, Gillespie JR, Creason SA, Huang W, Shibata S, Barros-Álvarez X, Verlinde CLMJ, Hol WGJ, Fan E, Buckner FS. Faghih O, et al. Among authors: creason sa. Antimicrob Agents Chemother. 2017 Oct 24;61(11):e00999-17. doi: 10.1128/AAC.00999-17. Print 2017 Nov. Antimicrob Agents Chemother. 2017. PMID: 28848016 Free PMC article.
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