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Easy-To-Synthesize Spirocyclic Compounds Possess Remarkable in Vivo Activity against Mycobacterium tuberculosis.
Guardia A, Baiget J, Cacho M, Pérez A, Ortega-Guerra M, Nxumalo W, Khanye SD, Rullas J, Ortega F, Jiménez E, Pérez-Herrán E, Fraile-Gabaldón MT, Esquivias J, Fernández R, Porras-De Francisco E, Encinas L, Alonso M, Giordano I, Rivero C, Miguel-Siles J, Osende JG, Badiola KA, Rutledge PJ, Todd MH, Remuiñán M, Alemparte C. Guardia A, et al. J Med Chem. 2018 Dec 27;61(24):11327-11340. doi: 10.1021/acs.jmedchem.8b01533. Epub 2018 Dec 12. J Med Chem. 2018. PMID: 30457865
Encoded library technology as a source of hits for the discovery and lead optimization of a potent and selective class of bactericidal direct inhibitors of Mycobacterium tuberculosis InhA.
Encinas L, O'Keefe H, Neu M, Remuiñán MJ, Patel AM, Guardia A, Davie CP, Pérez-Macías N, Yang H, Convery MA, Messer JA, Pérez-Herrán E, Centrella PA, Alvarez-Gómez D, Clark MA, Huss S, O'Donovan GK, Ortega-Muro F, McDowell W, Castañeda P, Arico-Muendel CC, Pajk S, Rullás J, Angulo-Barturen I, Alvarez-Ruíz E, Mendoza-Losana A, Ballell Pages L, Castro-Pichel J, Evindar G. Encinas L, et al. Among authors: guardia a. J Med Chem. 2014 Feb 27;57(4):1276-88. doi: 10.1021/jm401326j. Epub 2014 Feb 5. J Med Chem. 2014. PMID: 24450589
A Focused Screen Identifies Antifolates with Activity on Mycobacterium tuberculosis.
Kumar A, Guardia A, Colmenarejo G, Pérez E, Gonzalez RR, Torres P, Calvo D, Gómez RM, Ortega F, Jiménez E, Gabarro RC, Rullás J, Ballell L, Sherman DR. Kumar A, et al. Among authors: guardia a. ACS Infect Dis. 2015 Dec 11;1(12):604-14. doi: 10.1021/acsinfecdis.5b00063. Epub 2015 Aug 12. ACS Infect Dis. 2015. PMID: 26771003 Free PMC article.
N-Benzyl-4-((heteroaryl)methyl)benzamides: A New Class of Direct NADH-Dependent 2-trans Enoyl-Acyl Carrier Protein Reductase (InhA) Inhibitors with Antitubercular Activity.
Guardia A, Gulten G, Fernandez R, Gómez J, Wang F, Convery M, Blanco D, Martínez M, Pérez-Herrán E, Alonso M, Ortega F, Rullás J, Calvo D, Mata L, Young R, Sacchettini JC, Mendoza-Losana A, Remuiñán M, Ballell Pages L, Castro-Pichel J. Guardia A, et al. ChemMedChem. 2016 Apr 5;11(7):687-701. doi: 10.1002/cmdc.201600020. Epub 2016 Mar 2. ChemMedChem. 2016. PMID: 26934341
Exploring the SAR of the β-Ketoacyl-ACP Synthase Inhibitor GSK3011724A and Optimization around a Genotoxic Metabolite.
Cunningham F, Esquivias J, Fernández-Menéndez R, Pérez A, Guardia A, Escribano J, Rivero C, Vimal M, Cacho M, de Dios-Antón P, Martínez-Martínez MS, Jiménez E, Huertas Valentín L, Rebollo-López MJ, López-Román EM, Sousa-Morcuende V, Rullas J, Neu M, Chung CW, Bates RH. Cunningham F, et al. Among authors: guardia a. ACS Infect Dis. 2020 May 8;6(5):1098-1109. doi: 10.1021/acsinfecdis.9b00493. Epub 2020 Mar 20. ACS Infect Dis. 2020. PMID: 32196311
81 results