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A New Scalable Synthesis of ELQ-300, ELQ-316, and other Antiparasitic Quinolones.
Pou S, Dodean RA, Frueh L, Liebman KM, Gallagher RT, Jin H, Jacobs RT, Nilsen A, Stuart DR, Doggett JS, Riscoe MK, Winter RW. Pou S, et al. Org Process Res Dev. 2021 Aug 20;25(8):1841-1852. doi: 10.1021/acs.oprd.1c00099. Epub 2021 Aug 4. Org Process Res Dev. 2021. PMID: 35110959 Free PMC article.
ELQ-331 as a prototype for extremely durable chemoprotection against malaria.
Smilkstein MJ, Pou S, Krollenbrock A, Bleyle LA, Dodean RA, Frueh L, Hinrichs DJ, Li Y, Martinson T, Munar MY, Winter RW, Bruzual I, Whiteside S, Nilsen A, Koop DR, Kelly JX, Kappe SHI, Wilder BK, Riscoe MK. Smilkstein MJ, et al. Malar J. 2019 Aug 27;18(1):291. doi: 10.1186/s12936-019-2921-9. Malar J. 2019. PMID: 31455339 Free PMC article.
Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.
Dodean RA, Kancharla P, Li Y, Melendez V, Read L, Bane CE, Vesely B, Kreishman-Deitrick M, Black C, Li Q, Sciotti RJ, Olmeda R, Luong TL, Gaona H, Potter B, Sousa J, Marcsisin S, Caridha D, Xie L, Vuong C, Zeng Q, Zhang J, Zhang P, Lin H, Butler K, Roncal N, Gaynor-Ohnstad L, Leed SE, Nolan C, Huezo SJ, Rasmussen SA, Stephens MT, Tan JC, Cooper RA, Smilkstein MJ, Pou S, Winter RW, Riscoe MK, Kelly JX. Dodean RA, et al. J Med Chem. 2019 Apr 11;62(7):3475-3502. doi: 10.1021/acs.jmedchem.8b01961. Epub 2019 Mar 21. J Med Chem. 2019. PMID: 30852885 Free PMC article.
Targeted Structure-Activity Analysis of Endochin-like Quinolones Reveals Potent Qi and Qo Site Inhibitors of Toxoplasma gondii and Plasmodium falciparum Cytochrome bc1 and Identifies ELQ-400 as a Remarkably Effective Compound against Acute Experimental Toxoplasmosis.
McConnell EV, Bruzual I, Pou S, Winter R, Dodean RA, Smilkstein MJ, Krollenbrock A, Nilsen A, Zakharov LN, Riscoe MK, Doggett JS. McConnell EV, et al. ACS Infect Dis. 2018 Nov 9;4(11):1574-1584. doi: 10.1021/acsinfecdis.8b00133. Epub 2018 Aug 30. ACS Infect Dis. 2018. PMID: 30117728 Free PMC article.
Alkoxycarbonate Ester Prodrugs of Preclinical Drug Candidate ELQ-300 for Prophylaxis and Treatment of Malaria.
Frueh L, Li Y, Mather MW, Li Q, Pou S, Nilsen A, Winter RW, Forquer IP, Pershing AM, Xie LH, Smilkstein MJ, Caridha D, Koop DR, Campbell RF, Sciotti RJ, Kreishman-Deitrick M, Kelly JX, Vesely B, Vaidya AB, Riscoe MK. Frueh L, et al. ACS Infect Dis. 2017 Oct 13;3(10):728-735. doi: 10.1021/acsinfecdis.7b00062. Epub 2017 Sep 27. ACS Infect Dis. 2017. PMID: 28927276 Free PMC article.