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Modification of triclosan scaffold in search of improved inhibitors for enoyl-acyl carrier protein (ACP) reductase in Toxoplasma gondii.
Stec J, Fomovska A, Afanador GA, Muench SP, Zhou Y, Lai BS, El Bissati K, Hickman MR, Lee PJ, Leed SE, Auschwitz JM, Sommervile C, Woods S, Roberts CW, Rice D, Prigge ST, McLeod R, Kozikowski AP. Stec J, et al. Among authors: afanador ga. ChemMedChem. 2013 Jul;8(7):1138-60. doi: 10.1002/cmdc.201300050. Epub 2013 Jun 14. ChemMedChem. 2013. PMID: 23776166 Free PMC article.
Design, synthesis, and biological activity of diaryl ether inhibitors of Toxoplasma gondii enoyl reductase.
Cheng G, Muench SP, Zhou Y, Afanador GA, Mui EJ, Fomovska A, Lai BS, Prigge ST, Woods S, Roberts CW, Hickman MR, Lee PJ, Leed SE, Auschwitz JM, Rice DW, McLeod R. Cheng G, et al. Among authors: afanador ga. Bioorg Med Chem Lett. 2013 Apr 1;23(7):2035-43. doi: 10.1016/j.bmcl.2013.02.019. Epub 2013 Feb 13. Bioorg Med Chem Lett. 2013. PMID: 23453069 Free PMC article.
Discrimination of potent inhibitors of Toxoplasma gondii enoyl-acyl carrier protein reductase by a thermal shift assay.
Afanador GA, Muench SP, McPhillie M, Fomovska A, Schön A, Zhou Y, Cheng G, Stec J, Freundlich JS, Shieh HM, Anderson JW, Jacobus DP, Fidock DA, Kozikowski AP, Fishwick CW, Rice DW, Freire E, McLeod R, Prigge ST. Afanador GA, et al. Biochemistry. 2013 Dec 23;52(51):9155-66. doi: 10.1021/bi400945y. Epub 2013 Dec 13. Biochemistry. 2013. PMID: 24295325 Free PMC article.
The benzimidazole based drugs show good activity against T. gondii but poor activity against its proposed enoyl reductase enzyme target.
Wilkinson C, McPhillie MJ, Zhou Y, Woods S, Afanador GA, Rawson S, Khaliq F, Prigge ST, Roberts CW, Rice DW, McLeod R, Fishwick CW, Muench SP. Wilkinson C, et al. Among authors: afanador ga. Bioorg Med Chem Lett. 2014 Feb 1;24(3):911-6. doi: 10.1016/j.bmcl.2013.12.066. Epub 2013 Dec 22. Bioorg Med Chem Lett. 2014. PMID: 24398298 Free PMC article.
Novel N-benzoyl-2-hydroxybenzamide disrupts unique parasite secretory pathway.
Fomovska A, Huang Q, El Bissati K, Mui EJ, Witola WH, Cheng G, Zhou Y, Sommerville C, Roberts CW, Bettis S, Prigge ST, Afanador GA, Hickman MR, Lee PJ, Leed SE, Auschwitz JM, Pieroni M, Stec J, Muench SP, Rice DW, Kozikowski AP, McLeod R. Fomovska A, et al. Among authors: afanador ga. Antimicrob Agents Chemother. 2012 May;56(5):2666-82. doi: 10.1128/AAC.06450-11. Epub 2012 Feb 21. Antimicrob Agents Chemother. 2012. PMID: 22354304 Free PMC article.
13 results