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Hundreds of dual-stage antimalarial molecules discovered by a functional gametocyte screen.
Miguel-Blanco C, Molina I, Bardera AI, Díaz B, de Las Heras L, Lozano S, González C, Rodrigues J, Delves MJ, Ruecker A, Colmenarejo G, Viera S, Martínez-Martínez MS, Fernández E, Baum J, Sinden RE, Herreros E. Miguel-Blanco C, et al. Nat Commun. 2017 May 17;8:15160. doi: 10.1038/ncomms15160. Nat Commun. 2017. PMID: 28513586 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. 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. 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
Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity.
Kokkonda S, Deng X, White KL, Coteron JM, Marco M, de Las Heras L, White J, El Mazouni F, Tomchick DR, Manjalanagara K, Rudra KR, Chen G, Morizzi J, Ryan E, Kaminsky W, Leroy D, Martínez-Martínez MS, Jimenez-Diaz MB, Bazaga SF, Angulo-Barturen I, Waterson D, Burrows JN, Matthews D, Charman SA, Phillips MA, Rathod PK. Kokkonda S, et al. J Med Chem. 2016 Jun 9;59(11):5416-31. doi: 10.1021/acs.jmedchem.6b00275. Epub 2016 May 21. J Med Chem. 2016. PMID: 27127993 Free PMC article.
Identification of KasA as the cellular target of an anti-tubercular scaffold.
Abrahams KA, Chung CW, Ghidelli-Disse S, Rullas J, Rebollo-López MJ, Gurcha SS, Cox JA, Mendoza A, Jiménez-Navarro E, Martínez-Martínez MS, Neu M, Shillings A, Homes P, Argyrou A, Casanueva R, Loman NJ, Moynihan PJ, Lelièvre J, Selenski C, Axtman M, Kremer L, Bantscheff M, Angulo-Barturen I, Izquierdo MC, Cammack NC, Drewes G, Ballell L, Barros D, Besra GS, Bates RH. Abrahams KA, et al. Nat Commun. 2016 Sep 1;7:12581. doi: 10.1038/ncomms12581. Nat Commun. 2016. PMID: 27581223 Free PMC article.
A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance.
O'Neill PM, Amewu RK, Charman SA, Sabbani S, Gnädig NF, Straimer J, Fidock DA, Shore ER, Roberts NL, Wong MH, Hong WD, Pidathala C, Riley C, Murphy B, Aljayyoussi G, Gamo FJ, Sanz L, Rodrigues J, Cortes CG, Herreros E, Angulo-Barturén I, Jiménez-Díaz MB, Bazaga SF, Martínez-Martínez MS, Campo B, Sharma R, Ryan E, Shackleford DM, Campbell S, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Palmer MJ, Copple IM, Mercer AE, Ruecker A, Delves MJ, Sinden RE, Siegl P, Davies J, Rochford R, Kocken CHM, Zeeman AM, Nixon GL, Biagini GA, Ward SA. O'Neill PM, et al. Nat Commun. 2017 May 24;8:15159. doi: 10.1038/ncomms15159. Nat Commun. 2017. PMID: 28537265 Free PMC article.
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. 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
Development of a Highly Selective Plasmodium falciparum Proteasome Inhibitor with Anti-malaria Activity in Humanized Mice.
Zhan W, Zhang H, Ginn J, Leung A, Liu YJ, Michino M, Toita A, Okamoto R, Wong TT, Imaeda T, Hara R, Yukawa T, Chelebieva S, Tumwebaze PK, Lafuente-Monasterio MJ, Martinez-Martinez MS, Vendome J, Beuming T, Sato K, Aso K, Rosenthal PJ, Cooper RA, Meinke PT, Nathan CF, Kirkman LA, Lin G. Zhan W, et al. Angew Chem Int Ed Engl. 2021 Apr 19;60(17):9279-9283. doi: 10.1002/anie.202015845. Epub 2021 Mar 11. Angew Chem Int Ed Engl. 2021. PMID: 33433953 Free PMC article.
32 results