Page 86 - 81_04
P. 86
Tuberculosis is not an illness of the past 2009; 324: 801-4. b) Pasca MR, Degiacomi G, Ribeiro
AL, et al. Clinical isolates of Mycobacterium
44. Ma Z, Lienhardt C, McIlleron H, Nunn AJ, Wang X. tuberculosis in four European hospitals are uniformly
Global tuberculosis drug development pipeline: the susceptible to benzothiazinones. Antimicrob Agents
need and the reality. Lancet. 2010; 375: 2100-9. Chemother 2010; 54: 1616-18.
45. Sacksteder KA, Protopopova M, Barry CE, Andries K, 56. a) Boechat N, Ferreira VF, Ferreira SB, De Lourdes
Nacy CA. Discovery and development of SQ109: a GFM, et al. Novel 1,2,3-triazole derivatives for use
new antitubercular drug with a novel mechanism of against Mycobacterium tuberculosis H37Rv (ATCC
action. Future Microbiol 2012; 7: 823-37. 27294) strain. J Med Chem 2011; 54, 5988-99. b)
Lamichhane G. Novel targets in M. tuberculosis:
46. Bogatcheva E, Hanrahan C, Nikonenko B, et al. search for new drugs, Trends Mol Med 2011, 17: 25-
Identification of SQ609 as a lead compound from a 33.
library of dipiperidines. Bioorg Med Chem Lett 2011;
21: 5353-57. 57. Ver por ejemplo: a) Sullivan TJ, Truglio JJ, Boyne
ME, et al. High affinity InhA inhibitors with activity
47. Alffenaar JWC, van der Laan T, Simons S, et al. against drug-resistant strains of Mycobacterium
Susceptibility of Clinical Mycobacterium tuberculosis tuberculosis. ACS Chem Biol 2006; 1: 43-53. b)
isolates to a potentially less toxic derivate of linezolid, Vilcheze C, Baughn AD, Tufariello J, et al. Novel
PNU-100480. Antimicrob Agents Chemother 2011; inhibitors of InhA efficiently kill Mycobacterium
55: 1287-89. tuberculosis under aerobic and anaerobic conditions.
Antimicrob Agents Chemother 2011; 55: 3889-98. c)
48. Phase 2a EBA Trial of AZD5847. ClinicalTrials.gov Kinjo T, Koseki Y, Kobayashi M, et al. Identification
Identifier: NCT01516203. of compounds with potential antibacterial activity
against Mycobacterium through structure-based drug
49. Ananthan S, Faaleolea ER, Goldman RC, et al. High- screening. J Chem Inf Model 2013; 53: 1200-12.
throughput screening for inhibitors of Mycobacterium
tuberculosis H37Rv. Tuberculosis 2009; 89: 334-53. 58. Parikh SL, Xiao G, Tonge PJ. Inhibition of InhA, the
enoyl reductase from Mycobacterium tuberculosis, by
50. Dye C. Tuberculosis 2000-2010: control, but not triclosan and isoniazid. Biochemistry 2000; 39: 7645-
elimination. Int J Tuberc Lung Dis 2000; 4: S146– 50.
S152.
59. Wang F, Langley R, Gulten G, et al. Mechanism of
51. a) Elliott AM, Berning SE, Iseman MD, Peloquin CA. thioamide drug action against tuberculosis and
Failure of drug penetration and acquisition of drug leprosy. J Exp Med 2007; 204: 73-8.
resistance in chronic tuberculous empyema. Tuber
Lung Dis 1995; 76: 463–467. b) Wayne LG. 60. a) He X, Alian A, Stroud R, Ortiz de Montellano PR.
Dormancy of Mycobacterium tuberculosis and latency Pyrrolidine carboxamides as a novel class of inhibitors
of disease. Eur J Clin Microbiol Infect Dis 1994; 13: of enoyl acyl carrier protein reductase from
908-14. Mycobacterium tuberculosis. J Med Chem 2006; 49:
6308-23. b) Ballell L, Castro J, Fernandez R, et al.
52. Gillespie SH. Evolution of Drug Resistance in (Pyrazol-3-yl)-1,3,4-thiadiazole-2-amine and (pyrazol-
Mycobacterium tuberculosis: Clinical and Molecular 3-yl)-1,3,4-thiazole-2-amine compounds. World
Perspective. Antimicrob. Agents Chemother 2002; 46: Intellectual Property Organization 2010;
267-74. WO2010118852 A1.
53. a) Dinakaran M, Senthilkumar P, Yogeeswari P, et al. 61. a) Hartkoorn RC, Sala C, Neres J, et al. EMBO Mol
Novel ofloxacin derivatives: synthesis, Med 2012; 4: 1032-42. b) Avendaño C. Hacia un
antimycobacterial and toxicological evaluation. nuevo fármaco antituberculoso. Anales RANF? 2012;
Bioorg Med Chem Lett 2008; 18, 1229-36. b) Chopra 78: 288-97. c) Perryman AL, Yu W, Wang X, et al. A
S, Matsuyama K, Tran T, et al. Evaluation of gyrase B Virtual Screen Discovers Novel, Fragment-Sized
as a drug target in Mycobacterium tuberculosis. J Inhibitors of Mycobacterium tuberculosis InhA. J
Antimicrob Chemother 2012, 67: 415-21. c) Shirude Chem Inf Model 2015; 55: 645-59.
PS, Madhavapeddi P, Tucker JA, et al.
Aminopyrazinamides: novel and specific GyrB 62. Hartkoorn RC, Pojer F, Read JA, Gingell H, et al.
inhibitors that kill replicating and nonreplicating Pyridomycin bridges the NADH- and substrate-
Mycobacterium tuberculosis. ACS Chem Biol 2013; binding pockets of the enoyl reductase InhA. Nature
8: 519-23. d) Karkare S, Chung TT, Collin F, et al. Chem Biol 2014; 10: 96-99.
The naphthoquinone diospyrin is an inhibitor of DNA
gyrase with a novel mechanism of action. J Biol Chem 63. Ver: Altmann K-H, Horlacher O, Hartkoorn R, S
2013; 288: 5149-56. (inventors). Pyridomycin based compounds exhibiting
an antitubercular activity. Patente WO2014040709
54. McKee EE, Ferguson M, Bentley AT, Marks TA. A1, 20 Marzo de 2014.
Inhibition of mammalian mitochondrial protein
synthesis by oxazolidinones. Antimicrob Agents 64. a) Wolff KA, Nguyen L. Strategies for potentiation of
Chemother 2006; 50: 2042-49. ethionamide and folate antagonists against
55. Ver por ejemplo: a) Makarov V, Manina G, Mikusova 355
K, et al. Benzothiazinones kill Mycobacterium
tuberculosis by blocking arabinan synthesis. Science
@Real Academia Nacional de Farmacia. Spain