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Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium.
Cross RM, Flanigan DL, Monastyrskyi A, LaCrue AN, Sáenz FE, Maignan JR, Mutka TS, White KL, Shackleford DM, Bathurst I, Fronczek FR, Wojtas L, Guida WC, Charman SA, Burrows JN, Kyle DE, Manetsch R. Cross RM, et al. Among authors: bathurst i. J Med Chem. 2014 Nov 13;57(21):8860-79. doi: 10.1021/jm500942v. Epub 2014 Oct 22. J Med Chem. 2014. PMID: 25148516 Free PMC article.
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: bathurst i. 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.
Quinolone-3-diarylethers: a new class of antimalarial drug.
Nilsen A, LaCrue AN, White KL, Forquer IP, Cross RM, Marfurt J, Mather MW, Delves MJ, Shackleford DM, Saenz FE, Morrisey JM, Steuten J, Mutka T, Li Y, Wirjanata G, Ryan E, Duffy S, Kelly JX, Sebayang BF, Zeeman AM, Noviyanti R, Sinden RE, Kocken CHM, Price RN, Avery VM, Angulo-Barturen I, Jiménez-Díaz MB, Ferrer S, Herreros E, Sanz LM, Gamo FJ, Bathurst I, Burrows JN, Siegl P, Guy RK, Winter RW, Vaidya AB, Charman SA, Kyle DE, Manetsch R, Riscoe MK. Nilsen A, et al. Among authors: bathurst i. Sci Transl Med. 2013 Mar 20;5(177):177ra37. doi: 10.1126/scitranslmed.3005029. Sci Transl Med. 2013. PMID: 23515079 Free PMC article.
Discovery, synthesis, and optimization of antimalarial 4(1H)-quinolone-3-diarylethers.
Nilsen A, Miley GP, Forquer IP, Mather MW, Katneni K, Li Y, Pou S, Pershing AM, Stickles AM, Ryan E, Kelly JX, Doggett JS, White KL, Hinrichs DJ, Winter RW, Charman SA, Zakharov LN, Bathurst I, Burrows JN, Vaidya AB, Riscoe MK. Nilsen A, et al. Among authors: bathurst i. J Med Chem. 2014 May 8;57(9):3818-34. doi: 10.1021/jm500147k. Epub 2014 Apr 18. J Med Chem. 2014. PMID: 24720377 Free PMC article.
Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential.
Coteron JM, Marco M, Esquivias J, Deng X, White KL, White J, Koltun M, El Mazouni F, Kokkonda S, Katneni K, Bhamidipati R, Shackleford DM, Angulo-Barturen I, Ferrer SB, Jiménez-Díaz MB, Gamo FJ, Goldsmith EJ, Charman WN, Bathurst I, Floyd D, Matthews D, Burrows JN, Rathod PK, Charman SA, Phillips MA. Coteron JM, et al. Among authors: bathurst i. J Med Chem. 2011 Aug 11;54(15):5540-61. doi: 10.1021/jm200592f. Epub 2011 Jul 14. J Med Chem. 2011. PMID: 21696174 Free PMC article.
In vitro and in vivo characterization of the antimalarial lead compound SSJ-183 in Plasmodium models.
Schleiferböck S, Scheurer C, Ihara M, Itoh I, Bathurst I, Burrows JN, Fantauzzi P, Lotharius J, Charman SA, Morizzi J, Shackleford DM, White KL, Brun R, Wittlin S. Schleiferböck S, et al. Among authors: bathurst i. Drug Des Devel Ther. 2013 Nov 15;7:1377-84. doi: 10.2147/DDDT.S51298. eCollection 2013. Drug Des Devel Ther. 2013. PMID: 24255594 Free PMC article.
Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria.
Charman SA, Arbe-Barnes S, Bathurst IC, Brun R, Campbell M, Charman WN, Chiu FC, Chollet J, Craft JC, Creek DJ, Dong Y, Matile H, Maurer M, Morizzi J, Nguyen T, Papastogiannidis P, Scheurer C, Shackleford DM, Sriraghavan K, Stingelin L, Tang Y, Urwyler H, Wang X, White KL, Wittlin S, Zhou L, Vennerstrom JL. Charman SA, et al. Proc Natl Acad Sci U S A. 2011 Mar 15;108(11):4400-5. doi: 10.1073/pnas.1015762108. Epub 2011 Feb 7. Proc Natl Acad Sci U S A. 2011. PMID: 21300861 Free PMC article.
Central nervous system exposure of next generation quinoline methanols is reduced relative to mefloquine after intravenous dosing in mice.
Dow GS, Milner E, Bathurst I, Bhonsle J, Caridha D, Gardner S, Gerena L, Kozar M, Lanteri C, Mannila A, McCalmont W, Moon J, Read KD, Norval S, Roncal N, Shackleford DM, Sousa J, Steuten J, White KL, Zeng Q, Charman SA. Dow GS, et al. Among authors: bathurst i. Malar J. 2011 Jun 6;10:150. doi: 10.1186/1475-2875-10-150. Malar J. 2011. PMID: 21645370 Free PMC article.
Structure-activity relationships of 4-position diamine quinoline methanols as intermittent preventative treatment (IPT) against Plasmodium falciparum.
Milner E, Gardner S, Moon J, Grauer K, Auschwitz J, Bathurst I, Caridha D, Gerena L, Gettayacamin M, Johnson J, Kozar M, Lee P, Leed S, Li Q, McCalmont W, Melendez V, Roncal N, Sciotti R, Smith B, Sousa J, Tungtaeng A, Wipf P, Dow G. Milner E, et al. Among authors: bathurst i. J Med Chem. 2011 Sep 22;54(18):6277-85. doi: 10.1021/jm200647u. Epub 2011 Aug 22. J Med Chem. 2011. PMID: 21854078
76 results