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Design and Synthesis of Orally Bioavailable Piperazine Substituted 4(1H)-Quinolones with Potent Antimalarial Activity: Structure-Activity and Structure-Property Relationship Studies.
Neelarapu R, Maignan JR, Lichorowic CL, Monastyrskyi A, Mutka TS, LaCrue AN, Blake LD, Casandra D, Mashkouri S, Burrows JN, Willis PA, Kyle DE, Manetsch R. Neelarapu R, et al. Among authors: willis pa. J Med Chem. 2018 Feb 22;61(4):1450-1473. doi: 10.1021/acs.jmedchem.7b00738. Epub 2018 Feb 9. J Med Chem. 2018. PMID: 29215279 Free PMC article.
The Discovery of Novel Antimalarial Aminoxadiazoles as a Promising Nonendoperoxide Scaffold.
Sandoval E, Lafuente-Monasterio MJ, Almela MJ, Castañeda P, Jiménez Díaz MB, Martínez-Martínez MS, Vidal J, Angulo-Barturen Í, Bamborough P, Burrows J, Cammack N, Chaparro MJ, Coterón JM, de Cozar C, Crespo B, Díaz B, Drewes G, Fernández E, Ferrer-Bazaga S, Fraile MT, Gamo FJ, Ghidelli-Disse S, Gómez R, Haselden J, Huss S, León ML, de Mercado J, Macdonald SJF, Martín Hernando JI, Prats S, Puente M, Rodríguez A, de la Rosa JC, Rueda L, Selenski C, Willis P, Wilson DM, Witty M, Calderón F. Sandoval E, et al. J Med Chem. 2017 Aug 24;60(16):6880-6896. doi: 10.1021/acs.jmedchem.6b01441. Epub 2017 Aug 14. J Med Chem. 2017. PMID: 28806082
Antimalarial drug discovery - the path towards eradication.
Burrows JN, Burlot E, Campo B, Cherbuin S, Jeanneret S, Leroy D, Spangenberg T, Waterson D, Wells TN, Willis P. Burrows JN, et al. Parasitology. 2014 Jan;141(1):128-39. doi: 10.1017/S0031182013000826. Epub 2013 Jul 17. Parasitology. 2014. PMID: 23863111 Free PMC article. Review.
Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy.
Baragaña B, Norcross NR, Wilson C, Porzelle A, Hallyburton I, Grimaldi R, Osuna-Cabello M, Norval S, Riley J, Stojanovski L, Simeons FR, Wyatt PG, Delves MJ, Meister S, Duffy S, Avery VM, Winzeler EA, Sinden RE, Wittlin S, Frearson JA, Gray DW, Fairlamb AH, Waterson D, Campbell SF, Willis P, Read KD, Gilbert IH. Baragaña B, et al. J Med Chem. 2016 Nov 10;59(21):9672-9685. doi: 10.1021/acs.jmedchem.6b00723. Epub 2016 Sep 10. J Med Chem. 2016. PMID: 27631715 Free PMC article.
A novel multiple-stage antimalarial agent that inhibits protein synthesis.
Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A, Luksch T, Martínez MS, Luksch T, Bolscher JM, Woodland A, Norval S, Zuccotto F, Thomas J, Simeons F, Stojanovski L, Osuna-Cabello M, Brock PM, Churcher TS, Sala KA, Zakutansky SE, Jiménez-Díaz MB, Sanz LM, Riley J, Basak R, Campbell M, Avery VM, Sauerwein RW, Dechering KJ, Noviyanti R, Campo B, Frearson JA, Angulo-Barturen I, Ferrer-Bazaga S, Gamo FJ, Wyatt PG, Leroy D, Siegl P, Delves MJ, Kyle DE, Wittlin S, Marfurt J, Price RN, Sinden RE, Winzeler EA, Charman SA, Bebrevska L, Gray DW, Campbell S, Fairlamb AH, Willis PA, Rayner JC, Fidock DA, Read KD, Gilbert IH. Baragaña B, et al. Among authors: willis pa. Nature. 2015 Jun 18;522(7556):315-20. doi: 10.1038/nature14451. Nature. 2015. PMID: 26085270 Free PMC article.
Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials.
Norcross NR, Baragaña B, Wilson C, Hallyburton I, Osuna-Cabello M, Norval S, Riley J, Stojanovski L, Simeons FR, Porzelle A, Grimaldi R, Wittlin S, Duffy S, Avery VM, Meister S, Sanz L, Jiménez-Díaz B, Angulo-Barturen I, Ferrer S, Martínez MS, Gamo FJ, Frearson JA, Gray DW, Fairlamb AH, Winzeler EA, Waterson D, Campbell SF, Willis P, Read KD, Gilbert IH. Norcross NR, et al. J Med Chem. 2016 Jul 14;59(13):6101-20. doi: 10.1021/acs.jmedchem.6b00028. Epub 2016 Jun 17. J Med Chem. 2016. PMID: 27314305 Free PMC article.
72 results