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Items: 1 to 20 of 146

1.

Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis.

Makarov V, Manina G, Mikusova K, Möllmann U, Ryabova O, Saint-Joanis B, Dhar N, Pasca MR, Buroni S, Lucarelli AP, Milano A, De Rossi E, Belanova M, Bobovska A, Dianiskova P, Kordulakova J, Sala C, Fullam E, Schneider P, McKinney JD, Brodin P, Christophe T, Waddell S, Butcher P, Albrethsen J, Rosenkrands I, Brosch R, Nandi V, Bharath S, Gaonkar S, Shandil RK, Balasubramanian V, Balganesh T, Tyagi S, Grosset J, Riccardi G, Cole ST.

Science. 2009 May 8;324(5928):801-4. doi: 10.1126/science.1171583. Epub 2009 Mar 19.

2.

Clinical isolates of Mycobacterium tuberculosis in four European hospitals are uniformly susceptible to benzothiazinones.

Pasca MR, Degiacomi G, Ribeiro AL, Zara F, De Mori P, Heym B, Mirrione M, Brerra R, Pagani L, Pucillo L, Troupioti P, Makarov V, Cole ST, Riccardi G.

Antimicrob Agents Chemother. 2010 Apr;54(4):1616-8. doi: 10.1128/AAC.01676-09. Epub 2010 Jan 19.

3.

In vitro combination studies of benzothiazinone lead compound BTZ043 against Mycobacterium tuberculosis.

Lechartier B, Hartkoorn RC, Cole ST.

Antimicrob Agents Chemother. 2012 Nov;56(11):5790-3. doi: 10.1128/AAC.01476-12. Epub 2012 Aug 27.

4.

Towards a new combination therapy for tuberculosis with next generation benzothiazinones.

Makarov V, Lechartier B, Zhang M, Neres J, van der Sar AM, Raadsen SA, Hartkoorn RC, Ryabova OB, Vocat A, Decosterd LA, Widmer N, Buclin T, Bitter W, Andries K, Pojer F, Dyson PJ, Cole ST.

EMBO Mol Med. 2014 Mar;6(3):372-83. doi: 10.1002/emmm.201303575. Epub 2014 Feb 5.

5.

Decaprenylphosphoryl-β-D-ribose 2'-epimerase from Mycobacterium tuberculosis is a magic drug target.

Manina G, Pasca MR, Buroni S, De Rossi E, Riccardi G.

Curr Med Chem. 2010;17(27):3099-108. Review.

PMID:
20629622
6.

The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis.

Makarov V, Neres J, Hartkoorn RC, Ryabova OB, Kazakova E, Šarkan M, Huszár S, Piton J, Kolly GS, Vocat A, Conroy TM, Mikušová K, Cole ST.

Antimicrob Agents Chemother. 2015 Aug;59(8):4446-52. doi: 10.1128/AAC.00778-15. Epub 2015 May 18.

7.

Benzothiazinones: prodrugs that covalently modify the decaprenylphosphoryl-β-D-ribose 2'-epimerase DprE1 of Mycobacterium tuberculosis.

Trefzer C, Rengifo-Gonzalez M, Hinner MJ, Schneider P, Makarov V, Cole ST, Johnsson K.

J Am Chem Soc. 2010 Oct 6;132(39):13663-5. doi: 10.1021/ja106357w.

PMID:
20828197
8.

DprE1--from the discovery to the promising tuberculosis drug target.

Mikusová K, Makarov V, Neres J.

Curr Pharm Des. 2014;20(27):4379-403. Review.

PMID:
24245764
9.

Synthesis and structure-activity relationships evaluation of benzothiazinone derivatives as potential anti-tubercular agents.

Gao C, Ye TH, Wang NY, Zeng XX, Zhang LD, Xiong Y, You XY, Xia Y, Xu Y, Peng CT, Zuo WQ, Wei Y, Yu LT.

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4919-22. doi: 10.1016/j.bmcl.2013.06.069. Epub 2013 Jul 4.

PMID:
23886691
10.

Design, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moiety.

Lv K, Tao Z, Liu Q, Yang L, Wang B, Wu S, Wang A, Huang M, Liu M, Lu Y.

Eur J Med Chem. 2018 May 10;151:1-8. doi: 10.1016/j.ejmech.2018.03.060. Epub 2018 Mar 23.

PMID:
29601990
11.

Characterization of DprE1-Mediated Benzothiazinone Resistance in Mycobacterium tuberculosis.

Foo CS, Lechartier B, Kolly GS, Boy-Röttger S, Neres J, Rybniker J, Lupien A, Sala C, Piton J, Cole ST.

Antimicrob Agents Chemother. 2016 Oct 21;60(11):6451-6459. doi: 10.1128/AAC.01523-16. Print 2016 Nov.

12.

Antituberculars which target decaprenylphosphoryl-β-D-ribofuranose 2'-oxidase DprE1: state of art.

Buroni S, Pasca MR, de Jesus Lopes Ribeiro AL, Degiacomi G, Molteni E, Riccardi G.

Appl Microbiol Biotechnol. 2012 May;94(4):907-16. doi: 10.1007/s00253-012-4013-4. Epub 2012 Apr 18. Review. Retraction in: Appl Microbiol Biotechnol. 2012 Sep;95(5):1369.

PMID:
22526781
13.

Synthesis and antitubercular evaluation of 4-carbonyl piperazine substituted 1,3-benzothiazin-4-one derivatives.

Peng CT, Gao C, Wang NY, You XY, Zhang LD, Zhu YX, Xv Y, Zuo WQ, Ran K, Deng HX, Lei Q, Xiao KJ, Yu LT.

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1373-6. doi: 10.1016/j.bmcl.2015.02.061. Epub 2015 Mar 2.

PMID:
25754492
14.

Benzothiazinones mediate killing of Corynebacterineae by blocking decaprenyl phosphate recycling involved in cell wall biosynthesis.

Grover S, Alderwick LJ, Mishra AK, Krumbach K, Marienhagen J, Eggeling L, Bhatt A, Besra GS.

J Biol Chem. 2014 Feb 28;289(9):6177-87. doi: 10.1074/jbc.M113.522623. Epub 2014 Jan 20.

15.
16.

Tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide and N-benzyl-6',7'-dihydrospiro[piperidine-4,4'-thieno[3,2-c]pyran] analogues with bactericidal efficacy against Mycobacterium tuberculosis targeting MmpL3.

Remuiñán MJ, Pérez-Herrán E, Rullás J, Alemparte C, Martínez-Hoyos M, Dow DJ, Afari J, Mehta N, Esquivias J, Jiménez E, Ortega-Muro F, Fraile-Gabaldón MT, Spivey VL, Loman NJ, Pallen MJ, Constantinidou C, Minick DJ, Cacho M, Rebollo-López MJ, González C, Sousa V, Angulo-Barturen I, Mendoza-Losana A, Barros D, Besra GS, Ballell L, Cammack N.

PLoS One. 2013 Apr 17;8(4):e60933. doi: 10.1371/journal.pone.0060933. Print 2013.

17.

Design, syntheses, and anti-tuberculosis activities of conjugates of piperazino-1,3-benzothiazin-4-ones (pBTZs) with 2,7-dimethylimidazo [1,2-a]pyridine-3-carboxylic acids and 7-phenylacetyl cephalosporins.

Majewski MW, Tiwari R, Miller PA, Cho S, Franzblau SG, Miller MJ.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):2068-71. doi: 10.1016/j.bmcl.2016.02.076. Epub 2016 Feb 27.

18.

Analogous mechanisms of resistance to benzothiazinones and dinitrobenzamides in Mycobacterium smegmatis.

Ribeiro AL, Degiacomi G, Ewann F, Buroni S, Incandela ML, Chiarelli LR, Mori G, Kim J, Contreras-Dominguez M, Park YS, Han SJ, Brodin P, Valentini G, Rizzi M, Riccardi G, Pasca MR.

PLoS One. 2011;6(11):e26675. doi: 10.1371/journal.pone.0026675. Epub 2011 Nov 1.

19.

Structure, dynamics, and interaction of Mycobacterium tuberculosis (Mtb) DprE1 and DprE2 examined by molecular modeling, simulation, and electrostatic studies.

Bhutani I, Loharch S, Gupta P, Madathil R, Parkesh R.

PLoS One. 2015 Mar 19;10(3):e0119771. doi: 10.1371/journal.pone.0119771. eCollection 2015.

20.

Structural basis for benzothiazinone-mediated killing of Mycobacterium tuberculosis.

Neres J, Pojer F, Molteni E, Chiarelli LR, Dhar N, Boy-Röttger S, Buroni S, Fullam E, Degiacomi G, Lucarelli AP, Read RJ, Zanoni G, Edmondson DE, De Rossi E, Pasca MR, McKinney JD, Dyson PJ, Riccardi G, Mattevi A, Cole ST, Binda C.

Sci Transl Med. 2012 Sep 5;4(150):150ra121. doi: 10.1126/scitranslmed.3004395.

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