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Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice.
Gujjar R, El Mazouni F, White KL, White J, Creason S, Shackleford DM, Deng X, Charman WN, Bathurst I, Burrows J, Floyd DM, Matthews D, Buckner FS, Charman SA, Phillips MA, Rathod PK. Gujjar R, et al. J Med Chem. 2011 Jun 9;54(11):3935-49. doi: 10.1021/jm200265b. Epub 2011 May 12. J Med Chem. 2011. PMID: 21517059 Free PMC article.
Synthesis and Structure-Activity Relationships of the Novel Antimalarials 5-Pyridinyl-4(1 H)-Pyridones.
Bueno JM, Calderon F, Chicharro J, De la Rosa JC, Díaz B, Fernández J, Fiandor JM, Fraile MT, García M, Herreros E, García-Pérez A, Lorenzo M, Mallo A, Puente M, Saadeddin A, Ferrer S, Angulo-Barturen I, Burrows JN, León ML. Bueno JM, et al. Among authors: burrows jn. J Med Chem. 2018 Apr 26;61(8):3422-3435. doi: 10.1021/acs.jmedchem.7b01256. Epub 2018 Apr 5. J Med Chem. 2018. PMID: 29589932
Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential.
Coteron JM, Marco M, Esquivias J, Deng X, White KL, White J, Koltun M, El Mazouni F, Kokkonda S, Katneni K, Bhamidipati R, Shackleford DM, Angulo-Barturen I, Ferrer SB, Jiménez-Díaz MB, Gamo FJ, Goldsmith EJ, Charman WN, Bathurst I, Floyd D, Matthews D, Burrows JN, Rathod PK, Charman SA, Phillips MA. Coteron JM, et al. Among authors: burrows jn. J Med Chem. 2011 Aug 11;54(15):5540-61. doi: 10.1021/jm200592f. Epub 2011 Jul 14. J Med Chem. 2011. PMID: 21696174 Free PMC article.
Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series.
Palmer MJ, Deng X, Watts S, Krilov G, Gerasyuto A, Kokkonda S, El Mazouni F, White J, White KL, Striepen J, Bath J, Schindler KA, Yeo T, Shackleford DM, Mok S, Deni I, Lawong A, Huang A, Chen G, Wang W, Jayaseelan J, Katneni K, Patil R, Saunders J, Shahi SP, Chittimalla R, Angulo-Barturen I, Jiménez-Díaz MB, Wittlin S, Tumwebaze PK, Rosenthal PJ, Cooper RA, Aguiar ACC, Guido RVC, Pereira DB, Mittal N, Winzeler EA, Tomchick DR, Laleu B, Burrows JN, Rathod PK, Fidock DA, Charman SA, Phillips MA. Palmer MJ, et al. Among authors: burrows jn. J Med Chem. 2021 May 13;64(9):6085-6136. doi: 10.1021/acs.jmedchem.1c00173. Epub 2021 Apr 20. J Med Chem. 2021. PMID: 33876936 Free PMC article.
Novel orally active antimalarial thiazoles.
González Cabrera D, Douelle F, Feng TS, Nchinda AT, Younis Y, White KL, Wu Q, Ryan E, Burrows JN, Waterson D, Witty MJ, Wittlin S, Charman SA, Chibale K. González Cabrera D, et al. Among authors: burrows jn. J Med Chem. 2011 Nov 10;54(21):7713-9. doi: 10.1021/jm201108k. Epub 2011 Oct 11. J Med Chem. 2011. PMID: 21966980
Design and Synthesis of Orally Bioavailable Piperazine Substituted 4(1H)-Quinolones with Potent Antimalarial Activity: Structure-Activity and Structure-Property Relationship Studies.
Neelarapu R, Maignan JR, Lichorowic CL, Monastyrskyi A, Mutka TS, LaCrue AN, Blake LD, Casandra D, Mashkouri S, Burrows JN, Willis PA, Kyle DE, Manetsch R. Neelarapu R, et al. Among authors: burrows jn. J Med Chem. 2018 Feb 22;61(4):1450-1473. doi: 10.1021/acs.jmedchem.7b00738. Epub 2018 Feb 9. J Med Chem. 2018. PMID: 29215279 Free PMC article.
Discovery, synthesis, and optimization of antimalarial 4(1H)-quinolone-3-diarylethers.
Nilsen A, Miley GP, Forquer IP, Mather MW, Katneni K, Li Y, Pou S, Pershing AM, Stickles AM, Ryan E, Kelly JX, Doggett JS, White KL, Hinrichs DJ, Winter RW, Charman SA, Zakharov LN, Bathurst I, Burrows JN, Vaidya AB, Riscoe MK. Nilsen A, et al. Among authors: burrows jn. J Med Chem. 2014 May 8;57(9):3818-34. doi: 10.1021/jm500147k. Epub 2014 Apr 18. J Med Chem. 2014. PMID: 24720377 Free PMC article.
101 results