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A new in vivo screening paradigm to accelerate antimalarial drug discovery.
Jiménez-Díaz MB, Viera S, Ibáñez J, Mulet T, Magán-Marchal N, Garuti H, Gómez V, Cortés-Gil L, Martínez A, Ferrer S, Fraile MT, Calderón F, Fernández E, Shultz LD, Leroy D, Wilson DM, García-Bustos JF, Gamo FJ, Angulo-Barturen I. Jiménez-Díaz MB, et al. Among authors: calderon f. PLoS One. 2013 Jun 25;8(6):e66967. doi: 10.1371/journal.pone.0066967. Print 2013. PLoS One. 2013. PMID: 23825598 Free PMC article.
Case Study of Small Molecules As Antimalarials: 2-Amino-1-phenylethanol (APE) Derivatives.
Chaparro MJ, Vidal J, Angulo-Barturen I, Bueno JM, Burrows J, Cammack N, Castañeda P, Colmenarejo G, Coterón JM, de Las Heras L, Fernández E, Ferrer S, Gabarró R, Gamo FJ, García M, Jiménez-Díaz MB, Lafuente MJ, León ML, Martínez MS, Minick D, Prats S, Puente M, Rueda L, Sandoval E, Santos-Villarejo A, Witty M, Calderón F. Chaparro MJ, et al. Among authors: calderon f. ACS Med Chem Lett. 2014 Mar 26;5(6):657-61. doi: 10.1021/ml500015r. eCollection 2014 Jun 12. ACS Med Chem Lett. 2014. PMID: 24944739 Free PMC article.
A Developability-Focused Optimization Approach Allows Identification of in Vivo Fast-Acting Antimalarials: N-[3-[(Benzimidazol-2-yl)amino]propyl]amides.
Keurulainen L, Vahermo M, Puente-Felipe M, Sandoval-Izquierdo E, Crespo-Fernández B, Guijarro-López L, Huertas-Valentín L, de las Heras-Dueña L, Leino TO, Siiskonen A, Ballell-Pages L, Sanz LM, Castañeda-Casado P, Jiménez-Díaz MB, Martínez-Martínez MS, Viera S, Kiuru P, Calderón F, Yli-Kauhaluoma J. Keurulainen L, et al. Among authors: calderon f. J Med Chem. 2015 Jun 11;58(11):4573-80. doi: 10.1021/acs.jmedchem.5b00114. Epub 2015 May 19. J Med Chem. 2015. PMID: 25906200
Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials.
McConville M, Fernández J, Angulo-Barturen Í, Bahamontes-Rosa N, Ballell-Pages L, Castañeda P, de Cózar C, Crespo B, Guijarro L, Jiménez-Díaz MB, Martínez-Martínez MS, de Mercado J, Santos-Villarejo Á, Sanz LM, Frigerio M, Washbourn G, Ward SA, Nixon GL, Biagini GA, Berry NG, Blackman MJ, Calderón F, O'Neill PM. McConville M, et al. Among authors: calderon f. J Med Chem. 2015 Aug 27;58(16):6448-55. doi: 10.1021/acs.jmedchem.5b00434. Epub 2015 Aug 17. J Med Chem. 2015. PMID: 26222445
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. Among authors: calderon f. 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
Correction to 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. Among authors: calderon f. J Med Chem. 2017 Dec 14;60(23):9911. doi: 10.1021/acs.jmedchem.7b01491. Epub 2017 Nov 22. J Med Chem. 2017. PMID: 29164877 No abstract available.
204 results