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Page 1
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.
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.
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.
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
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.
Kokkonda S, Deng X, White KL, El Mazouni F, White J, Shackleford DM, Katneni K, Chiu FCK, Barker H, McLaren J, Crighton E, Chen G, Angulo-Barturen I, Jimenez-Diaz MB, Ferrer S, Huertas-Valentin L, Martinez-Martinez MS, Lafuente-Monasterio MJ, Chittimalla R, Shahi SP, Wittlin S, Waterson D, Burrows JN, Matthews D, Tomchick D, Rathod PK, Palmer MJ, Charman SA, Phillips MA. Kokkonda S, et al. J Med Chem. 2020 May 14;63(9):4929-4956. doi: 10.1021/acs.jmedchem.0c00311. Epub 2020 Apr 16. J Med Chem. 2020. PMID: 32248693 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
Hit-to-Lead Optimization of Benzoxazepinoindazoles As Human African Trypanosomiasis Therapeutics.
Klug DM, Tschiegg L, Diaz R, Rojas-Barros D, Perez-Moreno G, Ceballos G, García-Hernández R, Martinez-Martinez MS, Manzano P, Ruiz LM, Caffrey CR, Gamarro F, Pacanowska DG, Ferrins L, Navarro M, Pollastri MP. Klug DM, et al. J Med Chem. 2020 Mar 12;63(5):2527-2546. doi: 10.1021/acs.jmedchem.9b01506. Epub 2019 Nov 20. J Med Chem. 2020. PMID: 31670951 Free PMC article.
Lead Optimization of 3,5-Disubstituted-7-Azaindoles for the Treatment of Human African Trypanosomiasis.
Klug DM, Mavrogiannaki EM, Forbes KC, Silva L, Diaz-Gonzalez R, Pérez-Moreno G, Ceballos-Pérez G, Garcia-Hernández R, Bosch-Navarrete C, Cordón-Obras C, Gómez-Liñán C, Saura A, Momper JD, Martinez-Martinez MS, Manzano P, Syed A, El-Sakkary N, Caffrey CR, Gamarro F, Ruiz-Perez LM, Gonzalez Pacanowska D, Ferrins L, Navarro M, Pollastri MP. Klug DM, et al. Among authors: martinez martinez ms. J Med Chem. 2021 Jul 8;64(13):9404-9430. doi: 10.1021/acs.jmedchem.1c00674. Epub 2021 Jun 22. J Med Chem. 2021. PMID: 34156862 Free PMC article.
32 results