In vitro and in vivo profiles of ACH-702, an isothiazoloquinolone, against bacterial pathogens

Antimicrobial Agents and Chemotherapy

Volumn 55, Issue 6, 2011, Pages 2860-2871

  Pucci, Michael J ^a   Podos, Steven D ^a   Thanassi, Jane A ^a   Leggio, Melissa J ^a   Bradbury, Barton J ^a   Deshpande, Milind ^a,b  

^a Achillion Pharmaceuticals   (United States)

^b Rib X Pharmaceuticals   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACH 702; AMPICILLIN; ANTIBIOTIC AGENT; CEFTAZIDIME; CEFTRIAXONE; CHLORAMPHENICOL; CIPROFLOXACIN; CLINDAMYCIN; DNA TOPOISOMERASE (ATP HYDROLYSING); DNA TOPOISOMERASE IV; GEMIFLOXACIN; GENTAMICIN; IMIPENEM; LEVOFLOXACIN; LINEZOLID; MOXIFLOXACIN; OXACILLIN; PENICILLIN G; QUINOLONE DERIVATIVE; RIFAMPICIN; UNCLASSIFIED DRUG; VANCOMYCIN;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIBACTERIAL ACTIVITY; ANTIBIOTIC RESISTANCE; AREA UNDER THE CURVE; ARTICLE; BACTERIAL COLONIZATION; BACTERIAL MUTATION; BACTERIAL STRAIN; BACTERIUM ISOLATE; COLONY FORMING UNIT; CONTROLLED STUDY; DNA REPLICATION; DOSE RESPONSE; DRUG EFFICACY; DRUG POTENCY; DRUG STRUCTURE; ENZYME INHIBITION; EXPERIMENTAL INFECTION; FEMALE; GRAM NEGATIVE BACTERIUM; GRAM POSITIVE BACTERIUM; IN VITRO STUDY; IN VIVO STUDY; MAXIMUM PLASMA CONCENTRATION; METHICILLIN RESISTANT STAPHYLOCOCCUS AUREUS INFECTION; MINIMUM INHIBITORY CONCENTRATION; MOUSE; MYOSITIS; NONHUMAN; PRIORITY JOURNAL; SEPSIS; SINGLE DRUG DOSE; TIME TO MAXIMUM PLASMA CONCENTRATION;

ANIMALS; ANTI-BACTERIAL AGENTS; BACTERIA; DNA GYRASE; DNA REPLICATION; DNA TOPOISOMERASE IV; FEMALE; HUMANS; MICE; MICROBIAL SENSITIVITY TESTS; QUINOLONES; STAPHYLOCOCCUS AUREUS; THIAZOLES;

EID: 79956324409     PISSN: 00664804     EISSN: 10986596     Source Type: Journal    
DOI: 10.1128/AAC.01666-10     Document Type: Article

References (47)

1. Acar, J. F., and F. W. Goldstein. 1997. Trends in bacterial resistance to fluoroquinolones. Clin. Infect. Dis. 24(Suppl. 1):S67-S73.
2. Appelbaum, P. C. 2006. The emergence of vancomycin-intermediate and vancomycin-resistant Staphylococcus aureus. Clin. Microbiol. Infect. 12(Suppl. 1):16-23.
3. Arias, C., and B. Murray. 2009. Antibiotic-resistant bugs in the 21st century - a clinical super-challenge. N. Engl. J. Med. 360:439-443.
4. Bogdanovich, T., et al. 2005. Antistaphylococcal activity of DX-619, a new des-F(6)-quinolone, compared to those of other agents. Antimicrob. Agents Chemother. 49:3325-3333.
5. Boucher, H. W., et al. 2009. Bad bugs, no drugs: no ESKAPE! An update from the Infectious Diseases Society of America. Clin. Infect. Dis. 48:1-12.
6. Centers for Disease Control and Prevention. 1997. Update: Staphylococcus aureus with reduced susceptibility to vancomycin - United States, 1997. JAMA 278:1145-1146.
7. Centers for Disease Control and Prevention. 2002. Vancomycin resistant Staphylococcus aureus - Pennsylvania, 2002. JAMA 288:2116.
8. Chambers, H. F. 2005. Community-associated MRSA - resistance and virulence converge. N. Engl. J. Med. 352:2485-2487.
9. Cheng, J., et al. 2007. Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus. Antimicrob. Agents Chemother. 51:2445-2453. (Pubitemid 47047323)
10. Chu, D. T., P. B. Fernandes, A. K. Claiborne, L. Shen, and A. G. Pernet. 1988. Structure-activity relationships in quinolone antibacterials: design, synthesis, and biological activities of novel isothiazoloquinolones. Drugs Exp. Clin. Res. 14:379-383.
11. Chu, D. T., I. M. Lico, A. K. Claiborne, J. J. Plattner, and A. G. Pernet. 1990. Structure-activity relationship of quinolone antibacterial agents: the effects of C-2 substitution. Drugs Exp. Clin. Res. 16:215-224.
12. CLSI. 2006. Methods for dilution antimicrobial susceptibility tests for bacteria that grow aerobically, vol. 26, no. 2; approved standard, 7th ed. CLSI document M7-A7. CLSI, Wayne, PA.
13. CLSI. 2006. Methods for antimicrobial susceptibility testing of anaerobic bacteria, vol. 27, no. 2; approved standard, 7th ed. CLSI document M11-A7. CLSI, Wayne, PA.
14. CLSI. 2009. Performance standards for antimicrobial susceptibility testing; eighteenth informational supplement. CLSI document M100-S19. CLSI, Wayne, PA.
15. Courvalin, P. 2006. Vancomycin resistance in gram-positive cocci. Clin. Infect. Dis. 42(Suppl. 1):S25-S34.
16. Craig, W. A., and S. Gudmundsson. 1996. Postantibiotic effect, p. 296-329. In V. Lorian (ed.), Antibiotics in laboratory medicine. Williams and Wilkins Co., Baltimore, MD.
17. Giske, C. G., D. L. Monnet, O. Cars, and Y. Carmeli on behalf of ReACt-Action on Antibiotic Resistance. 2008. Clinical and economic impact of common multidrug-resistant gram-negative bacilli. Antimicrob. Agents Chemother. 52:813-821.
18. Hiramatsu, K., et al. 1997. Methicillin-resistant Staphylococcus aureus clinical strain with reduced vancomycin susceptibility. J. Antimicrob. Chemother. 40:135-136.
19. Hooper, D. C. 2002. Fluoroquinolone resistance among Gram-positive cocci. Lancet Infect. Dis. 2:530-538.
20. Ince, D., X. Zhang, and D. C. Hooper. 2003. Activity of and resistance to moxifloxacin in Staphylococcus aureus. Antimicrob. Agents Chemother. 47:1410-1415.
21. Ince, D., X. Zhang, L. C. Silver, D. C. Hooper. 2003. Topoisomerase targeting with and resistance to gemifloxacin in Staphylococcus aureus. Antimicrob. Agents Chemother. 47:274-282.
22. Jones, M. E., R. S. Blosser-Middleton, C. Thornsberry, J. A. Karlowsky, and D. F. Sahm. 2003. The activity of levofloxacin and other antimicrobials against clinical isolates of Streptococcus pneumoniae collected worldwide during 1999-2002. Diagn. Microbiol. Infect. Dis. 47:579-586.
23. Low, D. E., et al. 2002. Activity of BMS-284756, a novel des-fluoro(6) quinolone, against Staphylococcus aureus, including contributions of mutations to quinolone resistance. Antimicrob. Agents Chemother. 46:1119-1121.
24. Molina-Torres, C. A., J. Ocampo-Candiani, A. Rendón, M. J. Pucci, and L. Vera-Cabrera. 2010. In vitro activity of a new isothiazoloquinolone, ACH-702, against Mycobacterium tuberculosis and other mycobacteria. Antimicrob. Agents Chemother. 54:2188-2190.
25. Mouton, J. W., M. N. Dudley, O. Cars, H. Derendorf, and G. L. Drusano. 2005. Standardization of pharmacokinetic/pharmacodynamic (PK/PD) terminology for anti-infective drugs: an update. J. Antimicrob. Chemother. 55:601-607.
26. Murakami, K., and A. Tomasz. 1989. Involvement of multiple genetic determinants in high-level methicillin resistance in Staphylococcus aureus. J. Bacteriol. 171:874-879. (Pubitemid 19053483)
27. Mychajlonka, M., T. D. McDowell, and G. D. Shockman. 1980. Inhibition of peptidoglycan, ribonucleic acid, and protein synthesis in tolerant strains of Streptococcus mutans. Antimicrob. Agents Chemother. 17:572-582.
28. Pankuch, G. A., and P. C. Appelbaum. 2005. Postantibiotic effect of DX-619 against 16 gram-positive organisms. Antimicrob. Agents Chemother. 49:3963-3965.
29. Paterson, D. L., and R. A. Bonomo. 2005. Extended-spectrum beta-lactamases: a clinical update. Clin. Microbiol. Rev. 18:657-686.
30. Périchon, B., and P. Courvalin. 2009. VanA-type vancomycin-resistant Staphylococcus aureus. Antimicrob. Agents Chemother. 53:4580-4587.
31. Poole, K. 2004. Resistance to beta-lactam antibiotics. Cell. Mol. Life Sci. 61:2200-2223.
32. Pucci, M. J., et al. 2007. In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens. Antimicrob. Agents Chemother. 51:1259-1267.
33. Pucci, M. J., et al. 2008. Abstr. 48th Intersci. Conf. Antimicrob. Agents Chemother., abstr. F1-2021.
34. Pucci, M. J., M. Ackerman, J. A. Thanassi, C. M. Shoen, and M. H. Cynamon. 2010. In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates. Antimicrob. Agents Chemother. 54:3478-3480.
35. Ratnaraja, N. V., and P. M. Hawkey. 2008. Current challenges in treating MRSA: what are the options? Expert Rev. Anti Infect. Ther. 6:601-618.
36. Reinert, R. R. 2009. The antimicrobial resistance profile of Streptococcus pneumoniae. Clin. Microbiol. Infect. 15(Suppl.3):7-11.
37. Silver, L. L. 2007. Multi-targeting by monotherapeutic antibacterials. Nat. Rev. Drug Discov. 6:41-55.
38. Strahilevitz, J., Q. C. Truong-Bolduc, and D. C. Hooper. 2005. DX-619, a novel des-fluoro(6) quinolone manifesting low frequency of selection of resistant Staphylococcus aureus mutants: quinolone resistance beyond modification of type II topoisomerases. Antimicrob. Agents Chemother. 49:5051-5057.
39. Strahilevitz, J., Y. Onodera, and D. C. Hooper. 2006. An improved expression plasmid for affinity purification of Staphylococcus aureus gyrase A subunit. Protein Expr. Purif. 47:10-15.
40. Terleckyj, B., N. P. Willett, and G. D. Shockman. 1975. Growth of several strains of oral streptococci in a chemically defined medium. Infect. Immun. 11:649-655.
41. Thanassi, J. A., et al. 2008. Abstr. 48th Intersci. Conf. Antimicrob. Agents Chemother., abstr. F1-2022.
42. Vera-Cabrera, L., et al. 2010. In vitro activity of ACH-702, a new isothiazoloquinolone, against Nocardia brasiliensis compared with econazole and the carbapenems imipenem and meropenem alone or in combination with clavulanic acid. Antimicrob. Agents Chemother. 54:2191-2193.
43. Wang, Q., et al. 2007. Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions. J. Med. Chem. 50:199-210.
44. Wiles, J. A., et al. 2006. Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells. Bioorg. Med. Chem. Lett. 16:1272-1276.
45. Wiles, J. A., et al. 2006. Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: in vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus. Bioorg. Med. Chem. Lett. 16:1277-1281. (Pubitemid 43143005)
46. Yoshida, H., M. Bogaki, M. Nakamura, and S. Nakamura. 1990. Quinolone resistance-determining region in the DNA gyrA gene of Escherichia coli. Antimicrob. Agents Chemother. 34:1271-1272.
47. Zahar, J. R., et al. 2009. Addressing the challenge of extended-spectrum beta-lactamases. Curr. Opin. Investig. Drugs 10:172-180.