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Page 1
Pharmacological characterization, structural studies, and in vivo activities of anti-Chagas disease lead compounds derived from tipifarnib.
Buckner FS, Bahia MT, Suryadevara PK, White KL, Shackleford DM, Chennamaneni NK, Hulverson MA, Laydbak JU, Chatelain E, Scandale I, Verlinde CL, Charman SA, Lepesheva GI, Gelb MH. Buckner FS, et al. Among authors: white kl. Antimicrob Agents Chemother. 2012 Sep;56(9):4914-21. doi: 10.1128/AAC.06244-11. Epub 2012 Jul 9. Antimicrob Agents Chemother. 2012. PMID: 22777048 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: white kl. 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: white j, white kl. 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.
Antimalarial pyrido[1,2-a]benzimidazoles.
Ndakala AJ, Gessner RK, Gitari PW, October N, White KL, Hudson A, Fakorede F, Shackleford DM, Kaiser M, Yeates C, Charman SA, Chibale K. Ndakala AJ, et al. Among authors: white kl. J Med Chem. 2011 Jul 14;54(13):4581-9. doi: 10.1021/jm200227r. Epub 2011 Jun 16. J Med Chem. 2011. PMID: 21644541
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: white kl. Malar J. 2011 Jun 6;10:150. doi: 10.1186/1475-2875-10-150. Malar J. 2011. PMID: 21645370 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: white j, white kl. 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: white kl. 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: white kl. J Med Chem. 2012 Apr 12;55(7):3479-87. doi: 10.1021/jm3001373. Epub 2012 Mar 21. J Med Chem. 2012. PMID: 22390538
Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of Chagas disease.
Keenan M, Abbott MJ, Alexander PW, Armstrong T, Best WM, Berven B, Botero A, Chaplin JH, Charman SA, Chatelain E, von Geldern TW, Kerfoot M, Khong A, Nguyen T, McManus JD, Morizzi J, Ryan E, Scandale I, Thompson RA, Wang SZ, White KL. Keenan M, et al. Among authors: white kl. J Med Chem. 2012 May 10;55(9):4189-204. doi: 10.1021/jm2015809. Epub 2012 Apr 27. J Med Chem. 2012. PMID: 22536986
629 results