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Page 1
Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts.
Le Manach C, Dam J, Woodland JG, Kaur G, Khonde LP, Brunschwig C, Njoroge M, Wicht KJ, Horatscheck A, Paquet T, Boyle GA, Gibhard L, Taylor D, Lawrence N, Yeo T, Mok S, Eastman RT, Dorjsuren D, Talley DC, Guo H, Simeonov A, Reader J, van der Watt M, Erlank E, Venter N, Zawada JW, Aswat A, Nardini L, Coetzer TL, Lauterbach SB, Bezuidenhout BC, Theron A, Mancama D, Koekemoer LL, Birkholtz LM, Wittlin S, Delves M, Ottilie S, Winzeler EA, von Geldern TW, Smith D, Fidock DA, Street LJ, Basarab GS, Duffy J, Chibale K. Le Manach C, et al. Among authors: paquet t. J Med Chem. 2021 Feb 25;64(4):2291-2309. doi: 10.1021/acs.jmedchem.1c00034. Epub 2021 Feb 12. J Med Chem. 2021. PMID: 33573376
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: paquet t. J Med Chem. 2013 Nov 14;56(21):8860-71. doi: 10.1021/jm401278d. Epub 2013 Oct 29. J Med Chem. 2013. PMID: 24099149
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: paquet t. J Med Chem. 2014 Feb 13;57(3):1014-22. doi: 10.1021/jm401760c. Epub 2014 Jan 28. J Med Chem. 2014. PMID: 24446664
Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a softfocus kinase library: part 2.
Le Manach C, Paquet T, Gonzàlez Cabrera D, Younis Y, Taylor D, Wiesner L, Lawrence N, Schwager S, Waterson D, Witty MJ, Wittlin S, Street LJ, Chibale K. Le Manach C, et al. Among authors: paquet t. J Med Chem. 2014 Nov 13;57(21):8839-48. doi: 10.1021/jm500887k. Epub 2014 Oct 23. J Med Chem. 2014. PMID: 25313449
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: paquet t. 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 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: paquet t. 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
Potent Plasmodium falciparum gametocytocidal compounds identified by exploring the kinase inhibitor chemical space for dual active antimalarials.
van der Watt ME, Reader J, Churchyard A, Nondaba SH, Lauterbach SB, Niemand J, Abayomi S, van Biljon RA, Connacher JI, van Wyk RDJ, Le Manach C, Paquet T, González Cabrera D, Brunschwig C, Theron A, Lozano-Arias S, Rodrigues JFI, Herreros E, Leroy D, Duffy J, Street LJ, Chibale K, Mancama D, Coetzer TL, Birkholtz LM. van der Watt ME, et al. Among authors: paquet t. J Antimicrob Chemother. 2018 May 1;73(5):1279-1290. doi: 10.1093/jac/dky008. J Antimicrob Chemother. 2018. PMID: 29420756
Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγ null Mouse Model of Malaria.
Nchinda AT, Le Manach C, Paquet T, Gonzàlez Cabrera D, Wicht KJ, Brunschwig C, Njoroge M, Abay E, Taylor D, Lawrence N, Wittlin S, Jiménez-Díaz MB, Santos Martínez M, Ferrer S, Angulo-Barturen I, Lafuente-Monasterio MJ, Duffy J, Burrows J, Street LJ, Chibale K. Nchinda AT, et al. Among authors: paquet t. J Med Chem. 2018 May 10;61(9):4213-4227. doi: 10.1021/acs.jmedchem.8b00382. Epub 2018 Apr 27. J Med Chem. 2018. PMID: 29665687
34 results