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Optimization of physicochemical properties and safety profile of novel bacterial topoisomerase type II inhibitors (NBTIs) with activity against Pseudomonas aeruginosa.
Reck F, Ehmann DE, Dougherty TJ, Newman JV, Hopkins S, Stone G, Agrawal N, Ciaccio P, McNulty J, Barthlow H, O'Donnell J, Goteti K, Breen J, Comita-Prevoir J, Cornebise M, Cronin M, Eyermann CJ, Geng B, Carr GR, Pandarinathan L, Tang X, Cottone A, Zhao L, Bezdenejnih-Snyder N. Reck F, et al. Among authors: newman jv. Bioorg Med Chem. 2014 Oct 1;22(19):5392-409. doi: 10.1016/j.bmc.2014.07.040. Epub 2014 Aug 4. Bioorg Med Chem. 2014. PMID: 25155913
Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II: broad-spectrum antibacterial agents with reduced hERG activity.
Reck F, Alm R, Brassil P, Newman J, Dejonge B, Eyermann CJ, Breault G, Breen J, Comita-Prevoir J, Cronin M, Davis H, Ehmann D, Galullo V, Geng B, Grebe T, Morningstar M, Walker P, Hayter B, Fisher S. Reck F, et al. J Med Chem. 2011 Nov 24;54(22):7834-47. doi: 10.1021/jm2008826. Epub 2011 Oct 27. J Med Chem. 2011. PMID: 21999508
Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II with reduced pK(a): antibacterial agents with an improved safety profile.
Reck F, Alm RA, Brassil P, Newman JV, Ciaccio P, McNulty J, Barthlow H, Goteti K, Breen J, Comita-Prevoir J, Cronin M, Ehmann DE, Geng B, Godfrey AA, Fisher SL. Reck F, et al. Among authors: newman jv. J Med Chem. 2012 Aug 9;55(15):6916-33. doi: 10.1021/jm300690s. Epub 2012 Jul 20. J Med Chem. 2012. PMID: 22779424
In vivo validation of thymidylate kinase (TMK) with a rationally designed, selective antibacterial compound.
Keating TA, Newman JV, Olivier NB, Otterson LG, Andrews B, Boriack-Sjodin PA, Breen JN, Doig P, Dumas J, Gangl E, Green OM, Guler SY, Hentemann MF, Joseph-McCarthy D, Kawatkar S, Kutschke A, Loch JT, McKenzie AR, Pradeepan S, Prasad S, Martínez-Botella G. Keating TA, et al. Among authors: newman jv. ACS Chem Biol. 2012 Nov 16;7(11):1866-72. doi: 10.1021/cb300316n. Epub 2012 Aug 28. ACS Chem Biol. 2012. PMID: 22908966
Discovery of selective and potent inhibitors of gram-positive bacterial thymidylate kinase (TMK).
Martínez-Botella G, Breen JN, Duffy JE, Dumas J, Geng B, Gowers IK, Green OM, Guler S, Hentemann MF, Hernandez-Juan FA, Joseph-McCarthy D, Kawatkar S, Larsen NA, Lazari O, Loch JT, Macritchie JA, McKenzie AR, Newman JV, Olivier NB, Otterson LG, Owens AP, Read J, Sheppard DW, Keating TA. Martínez-Botella G, et al. Among authors: newman jv. J Med Chem. 2012 Nov 26;55(22):10010-21. doi: 10.1021/jm3011806. Epub 2012 Oct 24. J Med Chem. 2012. PMID: 23043329
Antibacterial inhibitors of Gram-positive thymidylate kinase: structure-activity relationships and chiral preference of a new hydrophobic binding region.
Kawatkar SP, Keating TA, Olivier NB, Breen JN, Green OM, Guler SY, Hentemann MF, Loch JT, McKenzie AR, Newman JV, Otterson LG, Martínez-Botella G. Kawatkar SP, et al. Among authors: newman jv. J Med Chem. 2014 Jun 12;57(11):4584-97. doi: 10.1021/jm500463c. Epub 2014 Jun 3. J Med Chem. 2014. PMID: 24828090
31 results