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Novel in vivo active anti-malarials based on a hydroxy-ethyl-amine scaffold.
Ciana CL, Siegrist R, Aissaoui H, Marx L, Racine S, Meyer S, Binkert C, de Kanter R, Fischli C, Wittlin S, Boss C. Ciana CL, et al. Among authors: wittlin s. Bioorg Med Chem Lett. 2013 Feb 1;23(3):658-62. doi: 10.1016/j.bmcl.2012.11.118. Epub 2012 Dec 11. Bioorg Med Chem Lett. 2013. PMID: 23260352
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: wittlin s. 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: wittlin s. J Med Chem. 2012 Apr 12;55(7):3479-87. doi: 10.1021/jm3001373. Epub 2012 Mar 21. J Med Chem. 2012. PMID: 22390538
Identification of a new chemical class of antimalarials.
Brunner R, Aissaoui H, Boss C, Bozdech Z, Brun R, Corminboeuf O, Delahaye S, Fischli C, Heidmann B, Kaiser M, Kamber J, Meyer S, Papastogiannidis P, Siegrist R, Voss T, Welford R, Wittlin S, Binkert C. Brunner R, et al. Among authors: wittlin s. J Infect Dis. 2012 Sep 1;206(5):735-43. doi: 10.1093/infdis/jis418. Epub 2012 Jun 25. J Infect Dis. 2012. PMID: 22732921
Structure-activity relationship studies of orally active antimalarial 3,5-substituted 2-aminopyridines.
González Cabrera D, Douelle F, Younis Y, Feng TS, Le Manach C, Nchinda AT, Street LJ, Scheurer C, Kamber J, White KL, Montagnat OD, Ryan E, Katneni K, Zabiulla KM, Joseph JT, Bashyam S, Waterson D, Witty MJ, Charman SA, Wittlin S, Chibale K. González Cabrera D, et al. Among authors: wittlin s. J Med Chem. 2012 Dec 27;55(24):11022-30. doi: 10.1021/jm301476b. Epub 2012 Dec 14. J Med Chem. 2012. PMID: 23189922
UV-triggered affinity capture identifies interactions between the Plasmodium falciparum multidrug resistance protein 1 (PfMDR1) and antimalarial agents in live parasitized cells.
Brunner R, Ng CL, Aissaoui H, Akabas MH, Boss C, Brun R, Callaghan PS, Corminboeuf O, Fidock DA, Frame IJ, Heidmann B, Le Bihan A, Jenö P, Mattheis C, Moes S, Müller IB, Paguio M, Roepe PD, Siegrist R, Voss T, Welford RW, Wittlin S, Binkert C. Brunner R, et al. Among authors: wittlin s. J Biol Chem. 2013 Aug 2;288(31):22576-83. doi: 10.1074/jbc.M113.453159. Epub 2013 Jun 10. J Biol Chem. 2013. PMID: 23754276 Free PMC article.
Inhibitors of plasmodial serine hydroxymethyltransferase (SHMT): cocrystal structures of pyrazolopyrans with potent blood- and liver-stage activities.
Witschel MC, Rottmann M, Schwab A, Leartsakulpanich U, Chitnumsub P, Seet M, Tonazzi S, Schwertz G, Stelzer F, Mietzner T, McNamara C, Thater F, Freymond C, Jaruwat A, Pinthong C, Riangrungroj P, Oufir M, Hamburger M, Mäser P, Sanz-Alonso LM, Charman S, Wittlin S, Yuthavong Y, Chaiyen P, Diederich F. Witschel MC, et al. Among authors: wittlin s. J Med Chem. 2015 Apr 9;58(7):3117-30. doi: 10.1021/jm501987h. Epub 2015 Mar 18. J Med Chem. 2015. PMID: 25785478
217 results