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Tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide and N-benzyl-6',7'-dihydrospiro[piperidine-4,4'-thieno[3,2-c]pyran] analogues with bactericidal efficacy against Mycobacterium tuberculosis targeting MmpL3.
Remuiñán MJ, Pérez-Herrán E, Rullás J, Alemparte C, Martínez-Hoyos M, Dow DJ, Afari J, Mehta N, Esquivias J, Jiménez E, Ortega-Muro F, Fraile-Gabaldón MT, Spivey VL, Loman NJ, Pallen MJ, Constantinidou C, Minick DJ, Cacho M, Rebollo-López MJ, González C, Sousa V, Angulo-Barturen I, Mendoza-Losana A, Barros D, Besra GS, Ballell L, Cammack N. Remuiñán MJ, et al. Among authors: cacho m. PLoS One. 2013 Apr 17;8(4):e60933. doi: 10.1371/journal.pone.0060933. Print 2013. PLoS One. 2013. PMID: 23613759 Free PMC article.
Mycobacterium tuberculosis gyrase inhibitors as a new class of antitubercular drugs.
Blanco D, Perez-Herran E, Cacho M, Ballell L, Castro J, González Del Río R, Lavandera JL, Remuiñán MJ, Richards C, Rullas J, Vázquez-Muñiz MJ, Woldu E, Zapatero-González MC, Angulo-Barturen I, Mendoza A, Barros D. Blanco D, et al. Among authors: cacho m. Antimicrob Agents Chemother. 2015 Apr;59(4):1868-75. doi: 10.1128/AAC.03913-14. Epub 2015 Jan 12. Antimicrob Agents Chemother. 2015. PMID: 25583730 Free PMC 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: cacho m. 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
Identification and Profiling of Hydantoins-A Novel Class of Potent Antimycobacterial DprE1 Inhibitors.
Rogacki MK, Pitta E, Balabon O, Huss S, Lopez-Roman EM, Argyrou A, Blanco-Ruano D, Cacho M, Vande Velde CML, Augustyns K, Ballell L, Barros D, Bates RH, Cunningham F, Van der Veken P. Rogacki MK, et al. Among authors: cacho m. J Med Chem. 2018 Dec 27;61(24):11221-11249. doi: 10.1021/acs.jmedchem.8b01356. Epub 2018 Dec 13. J Med Chem. 2018. PMID: 30500189
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: cacho m. 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.
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: cacho m. 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
Optimization of Hydantoins as Potent Antimycobacterial Decaprenylphosphoryl-β-d-Ribose Oxidase (DprE1) Inhibitors.
Balabon O, Pitta E, Rogacki MK, Meiler E, Casanueva R, Guijarro L, Huss S, Lopez-Roman EM, Santos-Villarejo Á, Augustyns K, Ballell L, Aguirre DB, Bates RH, Cunningham F, Cacho M, Van der Veken P. Balabon O, et al. Among authors: cacho m. J Med Chem. 2020 May 28;63(10):5367-5386. doi: 10.1021/acs.jmedchem.0c00107. Epub 2020 May 13. J Med Chem. 2020. PMID: 32342688
Identification of β-Lactams Active against Mycobacterium tuberculosis by a Consortium of Pharmaceutical Companies and Academic Institutions.
Gold B, Zhang J, Quezada LL, Roberts J, Ling Y, Wood M, Shinwari W, Goullieux L, Roubert C, Fraisse L, Bacqué E, Lagrange S, Filoche-Rommé B, Vieth M, Hipskind PA, Jungheim LN, Aubé J, Scarry SM, McDonald SL, Li K, Perkowski A, Nguyen Q, Dartois V, Zimmerman M, Olsen DB, Young K, Bonnett S, Joerss D, Parish T, Boshoff HI, Arora K, Barry CE 3rd, Guijarro L, Anca S, Rullas J, Rodríguez-Salguero B, Martínez-Martínez MS, Porras-De Francisco E, Cacho M, Barros-Aguirre D, Smith P, Berthel SJ, Nathan C, Bates RH. Gold B, et al. Among authors: cacho m. ACS Infect Dis. 2022 Mar 11;8(3):557-573. doi: 10.1021/acsinfecdis.1c00570. Epub 2022 Feb 22. ACS Infect Dis. 2022. PMID: 35192346 Free PMC article.
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