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Page 1
In vitro characterization of the antibacterial spectrum of novel bacterial type II topoisomerase inhibitors of the aminobenzimidazole class.
Mani N, Gross CH, Parsons JD, Hanzelka B, Müh U, Mullin S, Liao Y, Grillot AL, Stamos D, Charifson PS, Grossman TH. Mani N, et al. Among authors: charifson ps. Antimicrob Agents Chemother. 2006 Apr;50(4):1228-37. doi: 10.1128/AAC.50.4.1228-1237.2006. Antimicrob Agents Chemother. 2006. PMID: 16569833 Free PMC article.
Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships.
Charifson PS, Grillot AL, Grossman TH, Parsons JD, Badia M, Bellon S, Deininger DD, Drumm JE, Gross CH, LeTiran A, Liao Y, Mani N, Nicolau DP, Perola E, Ronkin S, Shannon D, Swenson LL, Tang Q, Tessier PR, Tian SK, Trudeau M, Wang T, Wei Y, Zhang H, Stamos D. Charifson PS, et al. J Med Chem. 2008 Sep 11;51(17):5243-63. doi: 10.1021/jm800318d. Epub 2008 Aug 9. J Med Chem. 2008. PMID: 18690678
Discovery of pyrazolthiazoles as novel and potent inhibitors of bacterial gyrase.
Ronkin SM, Badia M, Bellon S, Grillot AL, Gross CH, Grossman TH, Mani N, Parsons JD, Stamos D, Trudeau M, Wei Y, Charifson PS. Ronkin SM, et al. Among authors: charifson ps. Bioorg Med Chem Lett. 2010 May 1;20(9):2828-31. doi: 10.1016/j.bmcl.2010.03.052. Epub 2010 Mar 15. Bioorg Med Chem Lett. 2010. PMID: 20356737
Successful application of serum shift prediction models to the design of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV with improved in vivo efficacy.
Perola E, Stamos D, Grillot AL, Ronkin S, Wang T, LeTiran A, Tang Q, Deininger DD, Liao Y, Tian SK, Drumm JE, Nicolau DP, Tessier PR, Mani N, Grossman TH, Charifson PS. Perola E, et al. Among authors: charifson ps. Bioorg Med Chem Lett. 2014 May 1;24(9):2177-81. doi: 10.1016/j.bmcl.2014.03.022. Epub 2014 Mar 19. Bioorg Med Chem Lett. 2014. PMID: 24685546
Second-generation antibacterial benzimidazole ureas: discovery of a preclinical candidate with reduced metabolic liability.
Grillot AL, Le Tiran A, Shannon D, Krueger E, Liao Y, O'Dowd H, Tang Q, Ronkin S, Wang T, Waal N, Li P, Lauffer D, Sizensky E, Tanoury J, Perola E, Grossman TH, Doyle T, Hanzelka B, Jones S, Dixit V, Ewing N, Liao S, Boucher B, Jacobs M, Bennani Y, Charifson PS. Grillot AL, et al. Among authors: charifson ps. J Med Chem. 2014 Nov 13;57(21):8792-816. doi: 10.1021/jm500563g. Epub 2014 Oct 28. J Med Chem. 2014. PMID: 25317480
Active-site residues of Escherichia coli DNA gyrase required in coupling ATP hydrolysis to DNA supercoiling and amino acid substitutions leading to novobiocin resistance.
Gross CH, Parsons JD, Grossman TH, Charifson PS, Bellon S, Jernee J, Dwyer M, Chambers SP, Markland W, Botfield M, Raybuck SA. Gross CH, et al. Among authors: charifson ps. Antimicrob Agents Chemother. 2003 Mar;47(3):1037-46. doi: 10.1128/AAC.47.3.1037-1046.2003. Antimicrob Agents Chemother. 2003. PMID: 12604539 Free PMC article.
Crystal structures of Escherichia coli topoisomerase IV ParE subunit (24 and 43 kilodaltons): a single residue dictates differences in novobiocin potency against topoisomerase IV and DNA gyrase.
Bellon S, Parsons JD, Wei Y, Hayakawa K, Swenson LL, Charifson PS, Lippke JA, Aldape R, Gross CH. Bellon S, et al. Among authors: charifson ps. Antimicrob Agents Chemother. 2004 May;48(5):1856-64. doi: 10.1128/AAC.48.5.1856-1864.2004. Antimicrob Agents Chemother. 2004. PMID: 15105144 Free PMC article.
Design, synthesis and biological evaluation of potent NAD+-dependent DNA ligase inhibitors as potential antibacterial agents. Part 2: 4-amino-pyrido[2,3-d]pyrimidin-5(8H)-ones.
Wang T, Duncan L, Gu W, O'Dowd H, Wei Y, Perola E, Parsons J, Gross CH, Moody CS, Arends SJ, Charifson PS. Wang T, et al. Among authors: charifson ps. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3699-703. doi: 10.1016/j.bmcl.2012.04.038. Epub 2012 Apr 19. Bioorg Med Chem Lett. 2012. PMID: 22560470
Design, synthesis and biological evaluation of potent NAD+-dependent DNA ligase inhibitors as potential antibacterial agents. Part I: aminoalkoxypyrimidine carboxamides.
Gu W, Wang T, Maltais F, Ledford B, Kennedy J, Wei Y, Gross CH, Parsons J, Duncan L, Arends SJ, Moody C, Perola E, Green J, Charifson PS. Gu W, et al. Among authors: charifson ps. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3693-8. doi: 10.1016/j.bmcl.2012.04.037. Epub 2012 Apr 17. Bioorg Med Chem Lett. 2012. PMID: 22560473
50 results