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Page 1
SAR Studies of 5-Aminopyrazole-4-carboxamide Analogues as Potent and Selective Inhibitors of Toxoplasma gondii CDPK1.
Huang W, Ojo KK, Zhang Z, Rivas K, Vidadala RS, Scheele S, DeRocher AE, Choi R, Hulverson MA, Barrett LK, Bruzual I, Siddaramaiah LK, Kerchner KM, Kurnick MD, Freiberg GM, Kempf D, Hol WG, Merritt EA, Neckermann G, de Hostos EL, Isoherranen N, Maly DJ, Parsons M, Doggett JS, Van Voorhis WC, Fan E. Huang W, et al. Among authors: bruzual i. ACS Med Chem Lett. 2015 Oct 22;6(12):1184-1189. doi: 10.1021/acsmedchemlett.5b00319. eCollection 2015 Dec 10. ACS Med Chem Lett. 2015. PMID: 26693272 Free PMC article.
Development of an Orally Available and Central Nervous System (CNS) Penetrant Toxoplasma gondii Calcium-Dependent Protein Kinase 1 (TgCDPK1) Inhibitor with Minimal Human Ether-a-go-go-Related Gene (hERG) Activity for the Treatment of Toxoplasmosis.
Vidadala RS, Rivas KL, Ojo KK, Hulverson MA, Zambriski JA, Bruzual I, Schultz TL, Huang W, Zhang Z, Scheele S, DeRocher AE, Choi R, Barrett LK, Siddaramaiah LK, Hol WG, Fan E, Merritt EA, Parsons M, Freiberg G, Marsh K, Kempf DJ, Carruthers VB, Isoherranen N, Doggett JS, Van Voorhis WC, Maly DJ. Vidadala RS, et al. Among authors: bruzual i. J Med Chem. 2016 Jul 14;59(13):6531-46. doi: 10.1021/acs.jmedchem.6b00760. Epub 2016 Jul 1. J Med Chem. 2016. PMID: 27309760 Free PMC article.
Pharmacokinetics and In Vivo Efficacy of Pyrazolopyrimidine, Pyrrolopyrimidine, and 5-Aminopyrazole-4-Carboxamide Bumped Kinase Inhibitors against Toxoplasmosis.
Hulverson MA, Bruzual I, McConnell EV, Huang W, Vidadala RSR, Choi R, Arnold SLM, Whitman GR, McCloskey MC, Barrett LK, Rivas KL, Scheele S, DeRocher AE, Parsons M, Ojo KK, Maly DJ, Fan E, Van Voorhis WC, Doggett JS. Hulverson MA, et al. Among authors: bruzual i. J Infect Dis. 2019 Apr 16;219(9):1464-1473. doi: 10.1093/infdis/jiy664. J Infect Dis. 2019. PMID: 30423128 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. Among authors: bruzual i. 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.
Radical cure of experimental babesiosis in immunodeficient mice using a combination of an endochin-like quinolone and atovaquone.
Lawres LA, Garg A, Kumar V, Bruzual I, Forquer IP, Renard I, Virji AZ, Boulard P, Rodriguez EX, Allen AJ, Pou S, Wegmann KW, Winter RW, Nilsen A, Mao J, Preston DA, Belperron AA, Bockenstedt LK, Hinrichs DJ, Riscoe MK, Doggett JS, Ben Mamoun C. Lawres LA, et al. Among authors: bruzual i. J Exp Med. 2016 Jun 27;213(7):1307-18. doi: 10.1084/jem.20151519. Epub 2016 Jun 6. J Exp Med. 2016. PMID: 27270894 Free PMC article.
Antimalarial proteasome inhibitor reveals collateral sensitivity from intersubunit interactions and fitness cost of resistance.
Kirkman LA, Zhan W, Visone J, Dziedziech A, Singh PK, Fan H, Tong X, Bruzual I, Hara R, Kawasaki M, Imaeda T, Okamoto R, Sato K, Michino M, Alvaro EF, Guiang LF, Sanz L, Mota DJ, Govindasamy K, Wang R, Ling Y, Tumwebaze PK, Sukenick G, Shi L, Vendome J, Bhanot P, Rosenthal PJ, Aso K, Foley MA, Cooper RA, Kafsack B, Doggett JS, Nathan CF, Lin G. Kirkman LA, et al. Among authors: bruzual i. Proc Natl Acad Sci U S A. 2018 Jul 17;115(29):E6863-E6870. doi: 10.1073/pnas.1806109115. Epub 2018 Jul 2. Proc Natl Acad Sci U S A. 2018. PMID: 29967165 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. Among authors: bruzual i. Malar J. 2019 Aug 27;18(1):291. doi: 10.1186/s12936-019-2921-9. Malar J. 2019. PMID: 31455339 Free PMC article.
18 results