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Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials.
Kancharla P, Dodean RA, Li Y, Pou S, Pybus B, 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, Ceja FG, Rasmussen SA, Tumwebaze PK, Rosenthal PJ, Mu J, Bayles BR, Cooper RA, Reynolds KA, Smilkstein MJ, Riscoe MK, Kelly JX. Kancharla P, et al. Among authors: zeng q. J Med Chem. 2020 Jun 11;63(11):6179-6202. doi: 10.1021/acs.jmedchem.0c00539. Epub 2020 May 26. J Med Chem. 2020. PMID: 32390431 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. Among authors: zeng q. 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.
Tafenoquine and NPC-1161B require CYP 2D metabolism for anti-malarial activity: implications for the 8-aminoquinoline class of anti-malarial compounds.
Marcsisin SR, Sousa JC, Reichard GA, Caridha D, Zeng Q, Roncal N, McNulty R, Careagabarja J, Sciotti RJ, Bennett JW, Zottig VE, Deye G, Li Q, Read L, Hickman M, Dhammika Nanayakkara NP, Walker LA, Smith B, Melendez V, Pybus BS. Marcsisin SR, et al. Among authors: zeng q. Malar J. 2014 Jan 3;13:2. doi: 10.1186/1475-2875-13-2. Malar J. 2014. PMID: 24386891 Free PMC article.
Characterization of in vivo metabolites of WR319691, a novel compound with activity against Plasmodium falciparum.
Milner E, Sousa J, Pybus B, Melendez V, Gardner S, Grauer K, Moon J, Carroll D, Auschwitz J, Gettayacamin M, Lee P, Leed S, McCalmont W, Norval S, Tungtaeng A, Zeng Q, Kozar M, Read KD, Li Q, Dow G. Milner E, et al. Among authors: zeng q. Eur J Drug Metab Pharmacokinet. 2011 Sep;36(3):151-8. doi: 10.1007/s13318-011-0047-8. Epub 2011 Jul 13. Eur J Drug Metab Pharmacokinet. 2011. PMID: 21751074
The use of a prodrug approach to minimize potential CNS exposure of next generation quinoline methanols while maintaining efficacy in in vivo animal models.
Sousa JC, Milner E, Carroll D, McCalmont W, Gardner S, Moon J, Johnson JD, Lee P, Auschwitz J, Roncal N, Caridha D, Tungteung A, Zeng Q, Reyes S, Smith B, Li Q, Kozar MP, Melendez V, Dow G. Sousa JC, et al. Among authors: zeng q. Eur J Drug Metab Pharmacokinet. 2014 Dec;39(4):231-6. doi: 10.1007/s13318-013-0162-9. Epub 2014 Apr 7. Eur J Drug Metab Pharmacokinet. 2014. PMID: 24705994
7,141 results