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Page 1
Synthesis and biological activity of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. Part 2: 2'-substituted triclosan derivatives.
Freundlich JS, Yu M, Lucumi E, Kuo M, Tsai HC, Valderramos JC, Karagyozov L, Jacobs WR Jr, Schiehser GA, Fidock DA, Jacobus DP, Sacchettini JC. Freundlich JS, et al. Among authors: schiehser ga. Bioorg Med Chem Lett. 2006 Apr 15;16(8):2163-9. doi: 10.1016/j.bmcl.2006.01.051. Epub 2006 Feb 8. Bioorg Med Chem Lett. 2006. PMID: 16466916
Synthesis, biological activity, and X-ray crystal structural analysis of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. Part 1: 4'-substituted triclosan derivatives.
Freundlich JS, Anderson JW, Sarantakis D, Shieh HM, Yu M, Valderramos JC, Lucumi E, Kuo M, Jacobs WR Jr, Fidock DA, Schiehser GA, Jacobus DP, Sacchettini JC. Freundlich JS, et al. Among authors: schiehser ga. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5247-52. doi: 10.1016/j.bmcl.2005.08.044. Epub 2005 Sep 29. Bioorg Med Chem Lett. 2005. PMID: 16198563
X-ray structural analysis of Plasmodium falciparum enoyl acyl carrier protein reductase as a pathway toward the optimization of triclosan antimalarial efficacy.
Freundlich JS, Wang F, Tsai HC, Kuo M, Shieh HM, Anderson JW, Nkrumah LJ, Valderramos JC, Yu M, Kumar TR, Valderramos SG, Jacobs WR Jr, Schiehser GA, Jacobus DP, Fidock DA, Sacchettini JC. Freundlich JS, et al. Among authors: schiehser ga. J Biol Chem. 2007 Aug 31;282(35):25436-44. doi: 10.1074/jbc.M701813200. Epub 2007 Jun 13. J Biol Chem. 2007. PMID: 17567585 Free article.
Novel diaryl ureas with efficacy in a mouse model of malaria.
Anderson JW, Sarantakis D, Terpinski J, Kumar TR, Tsai HC, Kuo M, Ager AL, Jacobs WR Jr, Schiehser GA, Ekins S, Sacchettini JC, Jacobus DP, Fidock DA, Freundlich JS. Anderson JW, et al. Among authors: schiehser ga. Bioorg Med Chem Lett. 2013 Feb 15;23(4):1022-5. doi: 10.1016/j.bmcl.2012.12.022. Epub 2012 Dec 20. Bioorg Med Chem Lett. 2013. PMID: 23313245 Free PMC article.
The fatty acid biosynthesis enzyme FabI plays a key role in the development of liver-stage malarial parasites.
Yu M, Kumar TR, Nkrumah LJ, Coppi A, Retzlaff S, Li CD, Kelly BJ, Moura PA, Lakshmanan V, Freundlich JS, Valderramos JC, Vilcheze C, Siedner M, Tsai JH, Falkard B, Sidhu AB, Purcell LA, Gratraud P, Kremer L, Waters AP, Schiehser G, Jacobus DP, Janse CJ, Ager A, Jacobs WR Jr, Sacchettini JC, Heussler V, Sinnis P, Fidock DA. Yu M, et al. Cell Host Microbe. 2008 Dec 11;4(6):567-78. doi: 10.1016/j.chom.2008.11.001. Cell Host Microbe. 2008. PMID: 19064257 Free PMC article.
Lead Selection of a New Aminomethylphenol, JPC-3210, for Malaria Treatment and Prevention.
Chavchich M, Birrell GW, Ager AL, MacKenzie DO, Heffernan GD, Schiehser GA, Jacobus LR, Shanks GD, Jacobus DP, Edstein MD. Chavchich M, et al. Among authors: schiehser ga. Antimicrob Agents Chemother. 2016 Apr 22;60(5):3115-8. doi: 10.1128/AAC.03066-15. Print 2016 May. Antimicrob Agents Chemother. 2016. PMID: 26856849 Free PMC article.
JPC-2997, a new aminomethylphenol with high in vitro and in vivo antimalarial activities against blood stages of Plasmodium.
Birrell GW, Chavchich M, Ager AL, Shieh HM, Heffernan GD, Zhao W, Krasucki PE, Saionz KW, Terpinski J, Schiehser GA, Jacobus LR, Shanks GD, Jacobus DP, Edstein MD. Birrell GW, et al. Among authors: schiehser ga. Antimicrob Agents Chemother. 2015 Jan;59(1):170-7. doi: 10.1128/AAC.03762-14. Epub 2014 Oct 20. Antimicrob Agents Chemother. 2015. PMID: 25331702 Free PMC article.
Characterization of the Preclinical Pharmacology of the New 2-Aminomethylphenol, JPC-3210, for Malaria Treatment and Prevention.
Birrell GW, Heffernan GD, Schiehser GA, Anderson J, Ager AL, Morales P, MacKenzie D, van Breda K, Chavchich M, Jacobus LR, Shanks GD, Jacobus DP, Edstein MD. Birrell GW, et al. Among authors: schiehser ga. Antimicrob Agents Chemother. 2018 Mar 27;62(4):e01335-17. doi: 10.1128/AAC.01335-17. Print 2018 Apr. Antimicrob Agents Chemother. 2018. PMID: 29311093 Free PMC article.
19 results