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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. Makarov V, et al. Science. 2009 May 8;324(5928):801-4. doi: 10.1126/science.1171583. Epub 2009 Mar 19. Science. 2009. PMID: 19299584 Free PMC article.
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. Makarov V, et al. EMBO Mol Med. 2014 Mar;6(3):372-83. doi: 10.1002/emmm.201303575. Epub 2014 Feb 5. EMBO Mol Med. 2014. PMID: 24500695 Free PMC article.
Mechanism of action of 5-nitrothiophenes against Mycobacterium tuberculosis.
Hartkoorn RC, Ryabova OB, Chiarelli LR, Riccardi G, Makarov V, Cole ST. Hartkoorn RC, et al. Among authors: makarov v. Antimicrob Agents Chemother. 2014 May;58(5):2944-7. doi: 10.1128/AAC.02693-13. Epub 2014 Feb 18. Antimicrob Agents Chemother. 2014. PMID: 24550336 Free PMC article.
2-Carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1.
Neres J, Hartkoorn RC, Chiarelli LR, Gadupudi R, Pasca MR, Mori G, Venturelli A, Savina S, Makarov V, Kolly GS, Molteni E, Binda C, Dhar N, Ferrari S, Brodin P, Delorme V, Landry V, de Jesus Lopes Ribeiro AL, Farina D, Saxena P, Pojer F, Carta A, Luciani R, Porta A, Zanoni G, De Rossi E, Costi MP, Riccardi G, Cole ST. Neres J, et al. Among authors: makarov v. ACS Chem Biol. 2015 Mar 20;10(3):705-14. doi: 10.1021/cb5007163. Epub 2014 Dec 9. ACS Chem Biol. 2015. PMID: 25427196
Thiophenecarboxamide Derivatives Activated by EthA Kill Mycobacterium tuberculosis by Inhibiting the CTP Synthetase PyrG.
Mori G, Chiarelli LR, Esposito M, Makarov V, Bellinzoni M, Hartkoorn RC, Degiacomi G, Boldrin F, Ekins S, de Jesus Lopes Ribeiro AL, Marino LB, Centárová I, Svetlíková Z, Blaško J, Kazakova E, Lepioshkin A, Barilone N, Zanoni G, Porta A, Fondi M, Fani R, Baulard AR, Mikušová K, Alzari PM, Manganelli R, de Carvalho LP, Riccardi G, Cole ST, Pasca MR. Mori G, et al. Among authors: makarov v. Chem Biol. 2015 Jul 23;22(7):917-27. doi: 10.1016/j.chembiol.2015.05.016. Epub 2015 Jun 18. Chem Biol. 2015. PMID: 26097035 Free PMC article.
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. González-Martínez NA, et al. Among authors: makarov v. PLoS Negl Trop Dis. 2015 Oct 16;9(10):e0004022. doi: 10.1371/journal.pntd.0004022. eCollection 2015. PLoS Negl Trop Dis. 2015. PMID: 26474057 Free PMC article.
1,054 results