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The antimalarial MMV688533 provides potential for single-dose cures with a high barrier to Plasmodium falciparum parasite resistance.
Murithi JM, Pascal C, Bath J, Boulenc X, Gnädig NF, Pasaje CFA, Rubiano K, Yeo T, Mok S, Klieber S, Desert P, Jiménez-Díaz MB, Marfurt J, Rouillier M, Cherkaoui-Rbati MH, Gobeau N, Wittlin S, Uhlemann AC, Price RN, Wirjanata G, Noviyanti R, Tumwebaze P, Cooper RA, Rosenthal PJ, Sanz LM, Gamo FJ, Joseph J, Singh S, Bashyam S, Augereau JM, Giraud E, Bozec T, Vermat T, Tuffal G, Guillon JM, Menegotto J, Sallé L, Louit G, Cabanis MJ, Nicolas MF, Doubovetzky M, Merino R, Bessila N, Angulo-Barturen I, Baud D, Bebrevska L, Escudié F, Niles JC, Blasco B, Campbell S, Courtemanche G, Fraisse L, Pellet A, Fidock DA, Leroy D. Murithi JM, et al. Among authors: wittlin s. Sci Transl Med. 2021 Jul 21;13(603):eabg6013. doi: 10.1126/scitranslmed.abg6013. Sci Transl Med. 2021. PMID: 34290058 Free PMC article.
Discovery of dual function acridones as a new antimalarial chemotype.
Kelly JX, Smilkstein MJ, Brun R, Wittlin S, Cooper RA, Lane KD, Janowsky A, Johnson RA, Dodean RA, Winter R, Hinrichs DJ, Riscoe MK. Kelly JX, et al. Among authors: wittlin s. Nature. 2009 May 14;459(7244):270-3. doi: 10.1038/nature07937. Epub 2009 Apr 8. Nature. 2009. PMID: 19357645 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.
Triclosan is minimally effective in rodent malaria models.
Baschong W, Wittlin S, Inglis KA, Fairlamb AH, Croft SL, Kumar TR, Fidock DA, Brun R. Baschong W, et al. Among authors: wittlin s. Nat Med. 2011 Jan;17(1):33-4; author reply 34-5. doi: 10.1038/nm0111-33. Nat Med. 2011. PMID: 21217674 No abstract available.
Aminoindoles, a novel scaffold with potent activity against Plasmodium falciparum.
Barker RH Jr, Urgaonkar S, Mazitschek R, Celatka C, Skerlj R, Cortese JF, Tyndall E, Liu H, Cromwell M, Sidhu AB, Guerrero-Bravo JE, Crespo-Llado KN, Serrano AE, Lin JW, Janse CJ, Khan SM, Duraisingh M, Coleman BI, Angulo-Barturen I, Jiménez-Díaz MB, Magán N, Gomez V, Ferrer S, Martínez MS, Wittlin S, Papastogiannidis P, O'Shea T, Klinger JD, Bree M, Lee E, Levine M, Wiegand RC, Munoz B, Wirth DF, Clardy J, Bathurst I, Sybertz E. Barker RH Jr, et al. Among authors: wittlin s. Antimicrob Agents Chemother. 2011 Jun;55(6):2612-22. doi: 10.1128/AAC.01714-10. Epub 2011 Mar 21. Antimicrob Agents Chemother. 2011. PMID: 21422215 Free PMC article.
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
207 results