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Page 1
Identification of Selective Inhibitors of Plasmodium N-Myristoyltransferase by High-Throughput Screening.
Harupa A, De Las Heras L, Colmenarejo G, Lyons-Abbott S, Reers A, Caballero Hernandez I, Chung CW, Charter D, Myler PJ, Fernández-Menéndez RM, Calderón F, Palomo S, Rodríguez B, Berlanga M, Herreros-Avilés E, Staker BL, Fernández Álvaro E, Kaushansky A. Harupa A, et al. Among authors: fernandez menendez rm. J Med Chem. 2020 Jan 23;63(2):591-600. doi: 10.1021/acs.jmedchem.9b01343. Epub 2020 Jan 8. J Med Chem. 2020. PMID: 31850752
Screening of a Novel Fragment Library with Functional Complexity against Mycobacterium tuberculosis InhA.
Prati F, Zuccotto F, Fletcher D, Convery MA, Fernandez-Menendez R, Bates R, Encinas L, Zeng J, Chung CW, De Dios Anton P, Mendoza-Losana A, Mackenzie C, Green SR, Huggett M, Barros D, Wyatt PG, Ray PC. Prati F, et al. ChemMedChem. 2018 Apr 6;13(7):672-677. doi: 10.1002/cmdc.201700774. Epub 2018 Feb 19. ChemMedChem. 2018. PMID: 29399991 Free PMC article.
Discovery of heterocyclic replacements for the coumarin core of anti-tubercular FadD32 inhibitors.
Fang C, Lee KK, Nietupski R, Bates RH, Fernandez-Menendez R, Lopez-Roman EM, Guijarro-Lopez L, Yin Y, Peng Z, Gomez JE, Fisher S, Barros-Aguirre D, Hubbard BK, Serrano-Wu MH, Hung DT. Fang C, et al. Bioorg Med Chem Lett. 2018 Dec 1;28(22):3529-3533. doi: 10.1016/j.bmcl.2018.09.037. Epub 2018 Sep 29. Bioorg Med Chem Lett. 2018. PMID: 30316633 Free PMC article.
In vivo potent BM635 analogue with improved drug-like properties.
Poce G, Cocozza M, Alfonso S, Consalvi S, Venditti G, Fernandez-Menendez R, Bates RH, Barros Aguirre D, Ballell L, De Logu A, Vistoli G, Biava M. Poce G, et al. Eur J Med Chem. 2018 Feb 10;145:539-550. doi: 10.1016/j.ejmech.2017.12.075. Epub 2017 Dec 27. Eur J Med Chem. 2018. PMID: 29335214
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. 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
Design, synthesis, and evaluation of new thiadiazole-based direct inhibitors of enoyl acyl carrier protein reductase (InhA) for the treatment of tuberculosis.
Šink R, Sosič I, Živec M, Fernandez-Menendez R, Turk S, Pajk S, Alvarez-Gomez D, Lopez-Roman EM, Gonzales-Cortez C, Rullas-Triconado J, Angulo-Barturen I, Barros D, Ballell-Pages L, Young RJ, Encinas L, Gobec S. Šink R, et al. J Med Chem. 2015 Jan 22;58(2):613-24. doi: 10.1021/jm501029r. Epub 2014 Dec 29. J Med Chem. 2015. PMID: 25517015
Novel Pyrazole-Containing Compounds Active against Mycobacterium tuberculosis.
Poce G, Consalvi S, Venditti G, Alfonso S, Desideri N, Fernandez-Menendez R, Bates RH, Ballell L, Barros Aguirre D, Rullas J, De Logu A, Gardner M, Ioerger TR, Rubin EJ, Biava M. Poce G, et al. ACS Med Chem Lett. 2019 Sep 18;10(10):1423-1429. doi: 10.1021/acsmedchemlett.9b00204. eCollection 2019 Oct 10. ACS Med Chem Lett. 2019. PMID: 31620228 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. 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.
Pharmaceutical salt of BM635 with improved bioavailability.
Poce G, Consalvi S, Cocozza M, Fernandez-Menendez R, Bates RH, Ortega Muro F, Barros Aguirre D, Ballell L, Biava M. Poce G, et al. Eur J Pharm Sci. 2017 Mar 1;99:17-23. doi: 10.1016/j.ejps.2016.12.003. Epub 2016 Dec 8. Eur J Pharm Sci. 2017. PMID: 27939618