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Mycobacterium tuberculosis Decaprenylphosphoryl-β-d-ribose Oxidase Inhibitors: Expeditious Reconstruction of Suboptimal Hits into a Series with Potent in Vivo Activity.
Borthwick JA, Alemparte C, Wall I, Whitehurst BC, Argyrou A, Burley G, de Dios-Anton P, Guijarro L, Monteiro MC, Ortega F, Suckling CJ, Pichel JC, Cacho M, Young RJ. Borthwick JA, et al. Among authors: ortega f. J Med Chem. 2020 Mar 12;63(5):2557-2576. doi: 10.1021/acs.jmedchem.9b01561. Epub 2020 Jan 22. J Med Chem. 2020. PMID: 31922409 Free article.
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. Among authors: ortega guerra m, ortega f. 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
Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)-ol (GSK656).
Li X, Hernandez V, Rock FL, Choi W, Mak YSL, Mohan M, Mao W, Zhou Y, Easom EE, Plattner JJ, Zou W, Pérez-Herrán E, Giordano I, Mendoza-Losana A, Alemparte C, Rullas J, Angulo-Barturen I, Crouch S, Ortega F, Barros D, Alley MRK. Li X, et al. Among authors: ortega f. J Med Chem. 2017 Oct 12;60(19):8011-8026. doi: 10.1021/acs.jmedchem.7b00631. Epub 2017 Sep 27. J Med Chem. 2017. PMID: 28953378
MymA Bioactivated Thioalkylbenzoxazole Prodrug Family Active against Mycobacterium tuberculosis.
Moure AL, Narula G, Sorrentino F, Bojang A, Tsui CKM, Sao Emani C, Porras-De Francisco E, Díaz B, Rebollo-López MJ, Torres-Gómez PA, López-Román EM, Camino I, Casado Castro P, Guijarro López L, Ortega F, Ballell L, Barros-Aguirre D, Remuiñán Blanco M, Av-Gay Y. Moure AL, et al. Among authors: ortega f. J Med Chem. 2020 May 14;63(9):4732-4748. doi: 10.1021/acs.jmedchem.0c00003. Epub 2020 Apr 19. J Med Chem. 2020. PMID: 32275415
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. Among authors: ortega f. ChemMedChem. 2016 Apr 5;11(7):687-701. doi: 10.1002/cmdc.201600020. Epub 2016 Mar 2. ChemMedChem. 2016. PMID: 26934341
A Mycobacterium tuberculosis NBTI DNA Gyrase Inhibitor Is Active against Mycobacterium abscessus.
Ganapathy US, Del Río RG, Cacho-Izquierdo M, Ortega F, Lelièvre J, Barros-Aguirre D, Aragaw WW, Zimmerman MD, Lindman M, Dartois V, Gengenbacher M, Dick T. Ganapathy US, et al. Among authors: ortega f. Antimicrob Agents Chemother. 2021 Nov 17;65(12):e0151421. doi: 10.1128/AAC.01514-21. Epub 2021 Oct 4. Antimicrob Agents Chemother. 2021. PMID: 34606340 Free PMC article.
Antitubercular drugs for an old target: GSK693 as a promising InhA direct inhibitor.
Martínez-Hoyos M, Perez-Herran E, Gulten G, Encinas L, Álvarez-Gómez D, Alvarez E, Ferrer-Bazaga S, García-Pérez A, Ortega F, Angulo-Barturen I, Rullas-Trincado J, Blanco Ruano D, Torres P, Castañeda P, Huss S, Fernández Menéndez R, González Del Valle S, Ballell L, Barros D, Modha S, Dhar N, Signorino-Gelo F, McKinney JD, García-Bustos JF, Lavandera JL, Sacchettini JC, Jimenez MS, Martín-Casabona N, Castro-Pichel J, Mendoza-Losana A. Martínez-Hoyos M, et al. Among authors: ortega f. EBioMedicine. 2016 Jun;8:291-301. doi: 10.1016/j.ebiom.2016.05.006. Epub 2016 May 8. EBioMedicine. 2016. PMID: 27428438 Free PMC article.
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: ortega f. 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.
The multistate tuberculosis pharmacometric model: a semi-mechanistic pharmacokinetic-pharmacodynamic model for studying drug effects in an acute tuberculosis mouse model.
Chen C, Ortega F, Rullas J, Alameda L, Angulo-Barturen I, Ferrer S, Simonsson US. Chen C, et al. Among authors: ortega f. J Pharmacokinet Pharmacodyn. 2017 Apr;44(2):133-141. doi: 10.1007/s10928-017-9508-2. Epub 2017 Feb 15. J Pharmacokinet Pharmacodyn. 2017. PMID: 28205025 Free PMC article.
Assessing Pharmacodynamic Interactions in Mice Using the Multistate Tuberculosis Pharmacometric and General Pharmacodynamic Interaction Models.
Chen C, Wicha SG, de Knegt GJ, Ortega F, Alameda L, Sousa V, de Steenwinkel JEM, Simonsson USH. Chen C, et al. Among authors: ortega f. CPT Pharmacometrics Syst Pharmacol. 2017 Nov;6(11):787-797. doi: 10.1002/psp4.12226. Epub 2017 Oct 10. CPT Pharmacometrics Syst Pharmacol. 2017. PMID: 28657202 Free PMC article.
1,400 results