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Items: 1 to 20 of 110

1.

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.

2.

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.

3.

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.

4.

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.

5.

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.

6.

Optimized Background Regimen for Treatment of Active Tuberculosis with the Next-Generation Benzothiazinone Macozinone (PBTZ169).

Lupien A, Vocat A, Foo CS, Blattes E, Gillon JY, Makarov V, Cole ST.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e00840-18. doi: 10.1128/AAC.00840-18. Print 2018 Nov.

7.

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.

8.

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
9.

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.

10.

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
11.

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
12.

In Vivo Activity of the Benzothiazinones PBTZ169 and BTZ043 against Nocardia brasiliensis.

González-Martínez NA, Lozano-Garza HG, Castro-Garza J, De Osio-Cortez A, Vargas-Villarreal J, Cavazos-Rocha N, Ocampo-Candiani J, Makarov V, Cole ST, Vera-Cabrera L.

PLoS Negl Trop Dis. 2015 Oct 16;9(10):e0004022. doi: 10.1371/journal.pntd.0004022. eCollection 2015.

13.

Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents.

Wang A, Lv K, Tao Z, Gu J, Fu L, Liu M, Wan B, Franzblau SG, Ma C, Ma X, Han B, Wang A, Xu S, Lu Y.

Eur J Med Chem. 2019 Nov 1;181:111595. doi: 10.1016/j.ejmech.2019.111595. Epub 2019 Aug 6.

PMID:
31408806
14.

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.

15.

Mode of Action of Clofazimine and Combination Therapy with Benzothiazinones against Mycobacterium tuberculosis.

Lechartier B, Cole ST.

Antimicrob Agents Chemother. 2015 Aug;59(8):4457-63. doi: 10.1128/AAC.00395-15. Epub 2015 May 18.

16.

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
17.

Fluorescent Benzothiazinone Analogues Efficiently and Selectively Label Dpre1 in Mycobacteria and Actinobacteria.

Sommer R, Neres J, Piton J, Dhar N, van der Sar A, Mukherjee R, Laroche T, Dyson PJ, McKinney JD, Bitter W, Makarov V, Cole ST.

ACS Chem Biol. 2018 Nov 16;13(11):3184-3192. doi: 10.1021/acschembio.8b00790. Epub 2018 Oct 25.

PMID:
30289689
18.

In Vitro Activity of PBTZ169 against Multiple Mycobacterium Species.

Shi J, Lu J, Wen S, Zong Z, Huo F, Luo J, Liang Q, Li Y, Huang H, Pang Y.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01314-18. doi: 10.1128/AAC.01314-18. Print 2018 Nov.

19.

Structural studies of Mycobacterium tuberculosis DprE1 interacting with its inhibitors.

Piton J, Foo CS, Cole ST.

Drug Discov Today. 2017 Mar;22(3):526-533. doi: 10.1016/j.drudis.2016.09.014. Epub 2016 Sep 22. Review.

PMID:
27666194
20.

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.

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