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Items: 1 to 20 of 88

1.

Novel hydroxyl tricyclics (e.g., GSK966587) as potent inhibitors of bacterial type IIA topoisomerases.

Miles TJ, Hennessy AJ, Bax B, Brooks G, Brown BS, Brown P, Cailleau N, Chen D, Dabbs S, Davies DT, Esken JM, Giordano I, Hoover JL, Huang J, Jones GE, Sukmar SK, Spitzfaden C, Markwell RE, Minthorn EA, Rittenhouse S, Gwynn MN, Pearson ND.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5437-41. doi: 10.1016/j.bmcl.2013.07.013. Epub 2013 Jul 17.

PMID:
23968823
2.

Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.

Miles TJ, Axten JM, Barfoot C, Brooks G, Brown P, Chen D, Dabbs S, Davies DT, Downie DL, Eyrisch S, Gallagher T, Giordano I, Gwynn MN, Hennessy A, Hoover J, Huang J, Jones G, Markwell R, Miller WH, Minthorn EA, Rittenhouse S, Seefeld M, Pearson N.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7489-95. doi: 10.1016/j.bmcl.2011.09.117. Epub 2011 Oct 10.

PMID:
22047689
3.

Novel cyclohexyl-amides as potent antibacterials targeting bacterial type IIA topoisomerases.

Miles TJ, Barfoot C, Brooks G, Brown P, Chen D, Dabbs S, Davies DT, Downie DL, Eyrisch S, Giordano I, Gwynn MN, Hennessy A, Hoover J, Huang J, Jones G, Markwell R, Rittenhouse S, Xiang H, Pearson N.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7483-8. doi: 10.1016/j.bmcl.2011.09.114. Epub 2011 Oct 10.

PMID:
22030032
4.

Novel tricyclics (e.g., GSK945237) as potent inhibitors of bacterial type IIA topoisomerases.

Miles TJ, Hennessy AJ, Bax B, Brooks G, Brown BS, Brown P, Cailleau N, Chen D, Dabbs S, Davies DT, Esken JM, Giordano I, Hoover JL, Jones GE, Kusalakumari Sukmar SK, Markwell RE, Minthorn EA, Rittenhouse S, Gwynn MN, Pearson ND.

Bioorg Med Chem Lett. 2016 May 15;26(10):2464-2469. doi: 10.1016/j.bmcl.2016.03.106. Epub 2016 Mar 31.

PMID:
27055939
5.

Tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of left-hand-side moiety (Part-2).

Singh SB, Kaelin DE, Wu J, Miesel L, Tan CM, Black T, Nargund R, Meinke PT, Olsen DB, Lagrutta A, Lu J, Patel S, Rickert KW, Smith RF, Soisson S, Sherer E, Joyce LA, Wei C, Peng X, Wang X, Fukuda H, Kishii R, Takei M, Takano H, Shibasaki M, Yajima M, Nishimura A, Shibata T, Fukuda Y.

Bioorg Med Chem Lett. 2015 May 1;25(9):1831-5. doi: 10.1016/j.bmcl.2015.03.044. Epub 2015 Mar 24.

PMID:
25851938
6.

Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099).

Basarab GS, Hill PJ, Garner CE, Hull K, Green O, Sherer BA, Dangel PB, Manchester JI, Bist S, Hauck S, Zhou F, Uria-Nickelsen M, Illingworth R, Alm R, Rooney M, Eakin AE.

J Med Chem. 2014 Jul 24;57(14):6060-82. doi: 10.1021/jm500462x. Epub 2014 Jul 8.

PMID:
24959892
7.

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.

Bioorg Med Chem. 2014 Oct 1;22(19):5392-409. doi: 10.1016/j.bmc.2014.07.040. Epub 2014 Aug 4.

PMID:
25155913
8.

Fragment-to-hit-to-lead discovery of a novel pyridylurea scaffold of ATP competitive dual targeting type II topoisomerase inhibiting antibacterial agents.

Basarab GS, Manchester JI, Bist S, Boriack-Sjodin PA, Dangel B, Illingworth R, Sherer BA, Sriram S, Uria-Nickelsen M, Eakin AE.

J Med Chem. 2013 Nov 14;56(21):8712-35. doi: 10.1021/jm401208b. Epub 2013 Oct 29.

PMID:
24098982
9.

Pyrrolopyrimidine inhibitors of DNA gyrase B (GyrB) and topoisomerase IV (ParE), Part II: development of inhibitors with broad spectrum, Gram-negative antibacterial activity.

Trzoss M, Bensen DC, Li X, Chen Z, Lam T, Zhang J, Creighton CJ, Cunningham ML, Kwan B, Stidham M, Nelson K, Brown-Driver V, Castellano A, Shaw KJ, Lightstone FC, Wong SE, Nguyen TB, Finn J, Tari LW.

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1537-43. doi: 10.1016/j.bmcl.2012.11.073. Epub 2012 Dec 8.

PMID:
23294697
10.

Discovery of Novel DNA Gyrase Inhibiting Spiropyrimidinetriones: Benzisoxazole Fusion with N-Linked Oxazolidinone Substituents Leading to a Clinical Candidate (ETX0914).

Basarab GS, Doig P, Galullo V, Kern G, Kimzey A, Kutschke A, Newman JP, Morningstar M, Mueller J, Otterson L, Vishwanathan K, Zhou F, Gowravaram M.

J Med Chem. 2015 Aug 13;58(15):6264-82. doi: 10.1021/acs.jmedchem.5b00863. Epub 2015 Jul 24.

PMID:
26158756
11.

The chemistry and biological profile of trovafloxacin.

Brighty KE, Gootz TD.

J Antimicrob Chemother. 1997 Jun;39 Suppl B:1-14. Review.

PMID:
9222064
13.

Indole naphthyridinones as inhibitors of bacterial enoyl-ACP reductases FabI and FabK.

Seefeld MA, Miller WH, Newlander KA, Burgess WJ, DeWolf WE Jr, Elkins PA, Head MS, Jakas DR, Janson CA, Keller PM, Manley PJ, Moore TD, Payne DJ, Pearson S, Polizzi BJ, Qiu X, Rittenhouse SF, Uzinskas IN, Wallis NG, Huffman WF.

J Med Chem. 2003 Apr 24;46(9):1627-35.

PMID:
12699381
14.

Novel tetrahydropyran-based bacterial topoisomerase inhibitors with potent anti-gram positive activity and improved safety profile.

Surivet JP, Zumbrunn C, Rueedi G, Bur D, Bruyère T, Locher H, Ritz D, Seiler P, Kohl C, Ertel EA, Hess P, Gauvin JC, Mirre A, Kaegi V, Dos Santos M, Kraemer S, Gaertner M, Delers J, Enderlin-Paput M, Weiss M, Sube R, Hadana H, Keck W, Hubschwerlen C.

J Med Chem. 2015 Jan 22;58(2):927-42. doi: 10.1021/jm501590q. Epub 2014 Dec 23.

PMID:
25494934
15.

Novel compounds targeting bacterial DNA topoisomerase/DNA gyrase.

Ehmann DE, Lahiri SD.

Curr Opin Pharmacol. 2014 Oct;18:76-83. doi: 10.1016/j.coph.2014.09.007. Epub 2014 Sep 29. Review.

16.

Novel inhibitors of bacterial protein synthesis: structure-activity relationships for 1,8-naphthyridine derivatives incorporating position 3 and 4 variants.

Clark RF, Wang S, Ma Z, Weitzberg M, Motter C, Tufano M, Wagner R, Gu YG, Dandliker PJ, Lerner CG, Chovan LE, Cai Y, Black-Schaefer CL, Lynch L, Kalvin D, Nilius AM, Pratt SD, Soni N, Zhang T, Zhang X, Beutel BA.

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3299-302.

PMID:
15149694
17.

Exploring Left-Hand-Side substitutions in the benzoxazinone series of 4-amino-piperidine bacterial type IIa topoisomerase inhibitors.

Geng B, Comita-Prevoir J, Eyermann CJ, Reck F, Fisher S.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5432-5. doi: 10.1016/j.bmcl.2011.06.126. Epub 2011 Jul 2.

PMID:
21782427
18.

Improvement of the pharmacokinetics and in vivo antibacterial efficacy of a novel type IIa topoisomerase inhibitor by formulation in liposomes.

Shapiro AB, Newman J, Goteti K, Beaudoin ME, Harrison R, Hopkins S, Agrawal N, Rivin O.

Antimicrob Agents Chemother. 2013 Oct;57(10):4816-24. doi: 10.1128/AAC.00163-13. Epub 2013 Jul 22.

19.

Action of quinolones against Staphylococcus aureus topoisomerase IV: basis for DNA cleavage enhancement.

Anderson VE, Zaniewski RP, Kaczmarek FS, Gootz TD, Osheroff N.

Biochemistry. 2000 Mar 14;39(10):2726-32.

PMID:
10704224
20.

Synthesis and structure-activity relationships of 2-pyridones: a novel series of potent DNA gyrase inhibitors as antibacterial agents.

Li Q, Chu DT, Claiborne A, Cooper CS, Lee CM, Raye K, Berst KB, Donner P, Wang W, Hasvold L, Fung A, Ma Z, Tufano M, Flamm R, Shen LL, Baranowski J, Nilius A, Alder J, Meulbroek J, Marsh K, Crowell D, Hui Y, Seif L, Melcher LM, Plattner JJ, et al.

J Med Chem. 1996 Aug 2;39(16):3070-88.

PMID:
8759628

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