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A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria.
Phillips MA, Lotharius J, Marsh K, White J, Dayan A, White KL, Njoroge JW, El Mazouni F, Lao Y, Kokkonda S, Tomchick DR, Deng X, Laird T, Bhatia SN, March S, Ng CL, Fidock DA, Wittlin S, Lafuente-Monasterio M, Benito FJ, Alonso LM, Martinez MS, Jimenez-Diaz MB, Bazaga SF, Angulo-Barturen I, Haselden JN, Louttit J, Cui Y, Sridhar A, Zeeman AM, Kocken C, Sauerwein R, Dechering K, Avery VM, Duffy S, Delves M, Sinden R, Ruecker A, Wickham KS, Rochford R, Gahagen J, Iyer L, Riccio E, Mirsalis J, Bathhurst I, Rueckle T, Ding X, Campo B, Leroy D, Rogers MJ, Rathod PK, Burrows JN, Charman SA. Phillips MA, et al. Among authors: charman sa. Sci Transl Med. 2015 Jul 15;7(296):296ra111. doi: 10.1126/scitranslmed.aaa6645. Sci Transl Med. 2015. PMID: 26180101 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. Among authors: charman wn. 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.
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: charman wn, charman sa. 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.
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: charman wn, charman sa. 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.
Novel orally active antimalarial thiazoles.
González Cabrera D, Douelle F, Feng TS, Nchinda AT, Younis Y, White KL, Wu Q, Ryan E, Burrows JN, Waterson D, Witty MJ, Wittlin S, Charman SA, Chibale K. González Cabrera D, et al. Among authors: charman sa. J Med Chem. 2011 Nov 10;54(21):7713-9. doi: 10.1021/jm201108k. Epub 2011 Oct 11. J Med Chem. 2011. PMID: 21966980
3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential.
Younis Y, Douelle F, Feng TS, González Cabrera D, Le Manach C, Nchinda AT, Duffy S, White KL, Shackleford DM, Morizzi J, Mannila J, Katneni K, Bhamidipati R, Zabiulla KM, Joseph JT, Bashyam S, Waterson D, Witty MJ, Hardick D, Wittlin S, Avery V, Charman SA, Chibale K. Younis Y, et al. Among authors: charman sa. J Med Chem. 2012 Apr 12;55(7):3479-87. doi: 10.1021/jm3001373. Epub 2012 Mar 21. J Med Chem. 2012. PMID: 22390538
194 results