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Page 1
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: bashyam s. Sci Transl Med. 2021 Jul 21;13(603):eabg6013. doi: 10.1126/scitranslmed.abg6013. Sci Transl Med. 2021. PMID: 34290058 Free PMC article.
Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol.
Abla N, Bashyam S, Charman SA, Greco B, Hewitt P, Jiménez-Díaz MB, Katneni K, Kubas H, Picard D, Sambandan Y, Sanz L, Smith D, Wang T, Willis P, Wittlin S, Spangenberg T. Abla N, et al. Among authors: bashyam s. ACS Med Chem Lett. 2017 Nov 28;8(12):1304-1308. doi: 10.1021/acsmedchemlett.7b00391. eCollection 2017 Dec 14. ACS Med Chem Lett. 2017. PMID: 29259752 Free PMC article.
Identification of a Potential Antimalarial Drug Candidate from a Series of 2-Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle.
Le Manach C, Nchinda AT, Paquet T, Gonzàlez Cabrera D, Younis Y, Han Z, Bashyam S, Zabiulla M, Taylor D, Lawrence N, White KL, Charman SA, Waterson D, Witty MJ, Wittlin S, Botha ME, Nondaba SH, Reader J, Birkholtz LM, Jiménez-Díaz MB, Martínez MS, Ferrer S, Angulo-Barturen I, Meister S, Antonova-Koch Y, Winzeler EA, Street LJ, Chibale K. Le Manach C, et al. Among authors: bashyam s. J Med Chem. 2016 Nov 10;59(21):9890-9905. doi: 10.1021/acs.jmedchem.6b01265. Epub 2016 Oct 26. J Med Chem. 2016. PMID: 27748596
A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines.
Le Manach C, Paquet T, Brunschwig C, Njoroge M, Han Z, Gonzàlez Cabrera D, Bashyam S, Dhinakaran R, Taylor D, Reader J, Botha M, Churchyard A, Lauterbach S, Coetzer TL, Birkholtz LM, Meister S, Winzeler EA, Waterson D, Witty MJ, Wittlin S, Jiménez-Díaz MB, Santos Martínez M, Ferrer S, Angulo-Barturen I, Street LJ, Chibale K. Le Manach C, et al. Among authors: bashyam s. J Med Chem. 2015 Nov 12;58(21):8713-22. doi: 10.1021/acs.jmedchem.5b01605. Epub 2015 Nov 2. J Med Chem. 2015. PMID: 26502160
Identification and deconvolution of cross-resistance signals from antimalarial compounds using multidrug-resistant Plasmodium falciparum strains.
Chugh M, Scheurer C, Sax S, Bilsland E, van Schalkwyk DA, Wicht KJ, Hofmann N, Sharma A, Bashyam S, Singh S, Oliver SG, Egan TJ, Malhotra P, Sutherland CJ, Beck HP, Wittlin S, Spangenberg T, Ding XC. Chugh M, et al. Among authors: bashyam s. Antimicrob Agents Chemother. 2015 Feb;59(2):1110-8. doi: 10.1128/AAC.03265-14. Epub 2014 Dec 8. Antimicrob Agents Chemother. 2015. PMID: 25487796 Free PMC article.
2,4-Diaminothienopyrimidines as orally active antimalarial agents.
González Cabrera D, Le Manach C, Douelle F, Younis Y, Feng TS, Paquet T, Nchinda AT, Street LJ, Taylor D, de Kock C, Wiesner L, Duffy S, White KL, Zabiulla KM, Sambandan Y, Bashyam S, Waterson D, Witty MJ, Charman SA, Avery VM, Wittlin S, Chibale K. González Cabrera D, et al. Among authors: bashyam s. J Med Chem. 2014 Feb 13;57(3):1014-22. doi: 10.1021/jm401760c. Epub 2014 Jan 28. J Med Chem. 2014. PMID: 24446664
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: bashyam 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
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