Optimization of a novel potent and selective bacterial DNA helicase inhibitor scaffold from a high throughput screening hit

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 12, 2013, Pages 3481-3486

  Li, Bing ^a   Pai, Ramdas ^a   Aiello, Daniel ^a,b   Di, Ming ^a   Barnes, Marjorie H ^a   Peet, Norton P ^a   Bowlin, Terry L ^a   Moir, Donald T ^a  

^a MICROBIOTIX INC   (United States)

^b UNIVERSITY OF MASSACHUSETTS MEDICAL SCHOOL   (United States)

Author keywords

DNA helicase; DNA replication; Inhibitor; Optimization

Indexed keywords

BACTERIAL DNA HELICASE INHIBITOR; BENZOBISTHIAZOLE DERIVATIVE; ENZYME INHIBITOR; THIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; BACILLUS ANTHRACIS; CONTROLLED STUDY; DRUG POTENCY; DRUG SCREENING; ENZYME INHIBITION; HIGH THROUGHPUT SCREENING; NONHUMAN; STAPHYLOCOCCUS AUREUS;

ANTI-BACTERIAL AGENTS; BACILLUS ANTHRACIS; BACTERIAL PROTEINS; BENZOTHIAZOLES; DNA HELICASES; DNA, BACTERIAL; ENZYME INHIBITORS; HIGH-THROUGHPUT SCREENING ASSAYS; MICROBIAL SENSITIVITY TESTS; STAPHYLOCOCCUS AUREUS; STRUCTURE-ACTIVITY RELATIONSHIP;

BACILLUS ANTHRACIS; BACTERIA (MICROORGANISMS); STAPHYLOCOCCUS AUREUS;

EID: 84878115199     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.04.055     Document Type: Article

References (23)

1. G.J. Moran, A. Krishnadasan, R.J. Gorwitz, G.E. Fosheim, L.K. McDougal, R.B. Carey, and D.A. Talan N. Engl. J. Med. 355 2006 666
2. J.M. Streit, R.N. Jones, H.S. Sader, and T.R. Fritsche Int. J. Antimicrob. Agents 24 2004 111
3. F. Collin, S. Karkare, and A. Maxwell Appl. Microbiol. Biotechnol. 92 2011 479
4. J.M. Domagala, L.D. Hanna, C.L. Heifetz, M.P. Hutt, T.F. Mich, J.P. Sanchez, and M. Solomon J. Med. Chem. 29 1986 394
5. M.M. Butler, L.W. Dudycz, N.N. Khan, G.E. Wright, and N.C. Brown Nucleic Acids Res. 18 1990 7381
6. M.M. Butler, D.J. Skow, R.O. Stephenson, P.T. Lyden, W.A. LaMarr, and K.A. Foster Antimicrob. Agents Chemother. 46 2002 3770
7. P.M. Tarantino Jr., C. Zhi, G.E. Wright, and N.C. Brown Antimicrob. Agents Chemother. 1999 1982 43
8. S.S. Patel, and K.M. Picha Annu. Rev. Biochem. 69 2000 651
9. S.E. Moyer, P.W. Lewis, and M.R. Botchan Proc. Natl. Acad. Sci. U.S.A. 103 2006 10236
10. S. Dubaele, W. Jahnke, J. Schoepfer, J. Fuchs, and P. Chene Bioorg. Med. Chem. Lett. 16 2006 923
11. D.L. Earnshaw, K.J. Moore, C.J. Greenwood, H. Djaballah, A.J. Jurewicz, K.J. Murray, and A.J. Pope J. Biomol. Screen. 4 1999 239
12. D.L. Earnshaw, and A.J. Pope J. Biomol. Screen. 6 2001 39
13. M.A. Griep, S. Blood, M.A. Larson, S.A. Koepsell, and S.H. Hinrichs Bioorg. Med. Chem. 15 2007 7203
14. G.A. McKay, R. Reddy, F. Arhin, A. Belley, D. Lehoux, G. Moeck, I. Sarmiento, T.R. Parr, P. Gros, J. Pelletier, and A.R. Far Bioorg. Med. Chem. Lett. 16 2006 1286
15. B. Zhang, A.H. Zhang, L. Chen, and X.G. Xi J. Biochem. 143 2008 773
16. L. Zhang, G. Schwartz, M. O'Donnell, and R.K. Harrison Anal. Biochem. 293 2001 31
17. Y. Zhang, F. Yang, Y.C. Kao, M.G. Kurilla, D.L. Pompliano, and I.B. Dicker Anal. Biochem. 304 2002 174
18. S. Bailey, W.K. Eliason, and T.A. Steitz Science 318 2007 459
19. O. Itsathitphaisarn, R.A. Wing, W.K. Eliason, J. Wang, and T.A. Steitz Cell 151 2012 267
20. D. Aiello, M.H. Barnes, E.E. Biswas, S.B. Biswas, S. Gu, J.D. Williams, T.L. Bowlin, and D.T. Moir Bioorg. Med. Chem. 17 2009 4466
21. B. Li, R. Pai, M. Di, D. Aiello, M.M. Butler, T. Tashjian, N.P. Peet, T.L. Bowlin, and D. Moir J. Med. Chem. 55 2012 10896
22. M. Wei, R. Wynn, G. Hollis, B. Liao, A. Margulis, B.G. Reid, R. Klabe, P.C. Liu, M. Becker-Pasha, M. Rupar, T.C. Burn, D.E. McCall, and Y. Li J. Biomol. Screen. 12 2007 220
23. N.C. Brown, C.L. Weisseman III, and T. Matsushita Nat. New Biol. 237 1972 72