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Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model.
Horatscheck A, Andrijevic A, Nchinda AT, Le Manach C, Paquet T, Khonde LP, Dam J, Pawar K, Taylor D, Lawrence N, Brunschwig C, Gibhard L, Njoroge M, Reader J, van der Watt M, Wicht K, de Sousa ACC, Okombo J, Maepa K, Egan TJ, Birkholtz LM, Basarab GS, Wittlin S, Fish PV, Street LJ, Duffy J, Chibale K. Horatscheck A, et al. Among authors: wittlin s. J Med Chem. 2020 Nov 12;63(21):13013-13030. doi: 10.1021/acs.jmedchem.0c01411. Epub 2020 Oct 25. J Med Chem. 2020. PMID: 33103428 Free PMC article.
Novel inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with anti-malarial activity in the mouse model.
Booker ML, Bastos CM, Kramer ML, Barker RH Jr, Skerlj R, Sidhu AB, Deng X, Celatka C, Cortese JF, Guerrero Bravo JE, Crespo Llado KN, Serrano AE, Angulo-Barturen I, Jiménez-Díaz MB, Viera S, Garuti H, Wittlin S, Papastogiannidis P, Lin JW, Janse CJ, Khan SM, Duraisingh M, Coleman B, Goldsmith EJ, Phillips MA, Munoz B, Wirth DF, Klinger JD, Wiegand R, Sybertz E. Booker ML, et al. Among authors: wittlin s. J Biol Chem. 2010 Oct 22;285(43):33054-33064. doi: 10.1074/jbc.M110.162081. Epub 2010 Aug 11. J Biol Chem. 2010. PMID: 20702404 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: 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
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.
Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity.
Younis Y, Douelle F, González Cabrera D, Le Manach C, Nchinda AT, Paquet T, Street LJ, White KL, Zabiulla KM, Joseph JT, Bashyam S, Waterson D, Witty MJ, Wittlin S, Charman SA, Chibale K. Younis Y, et al. Among authors: wittlin s. J Med Chem. 2013 Nov 14;56(21):8860-71. doi: 10.1021/jm401278d. Epub 2013 Oct 29. J Med Chem. 2013. PMID: 24099149
209 results