Design, synthesis and antibacterial activity studies of thiazole derivatives as potent ecKAS III inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 14, 2013, Pages 4235-4238

  Cheng, Kui ^a   Xue, Jia Yu ^a   Zhu, Hai Liang ^a  

^a NANJING UNIVERSITY   (China)

Author keywords

Amide ecKAS III inhibitors; Antibacterial; Computer simulation; Thiazole derivatives

Indexed keywords

3 OXOACYL ACYL CARRIER PROTEIN SYNTHASE; ACYLTRANSFERASE INHIBITOR; THIAZOLE DERIVATIVE;

ANTIBACTERIAL ACTIVITY; ARTICLE; BACILLUS SUBTILIS; CELL SURVIVAL; CONCENTRATION RESPONSE; DRUG DESIGN; DRUG STRUCTURE; DRUG SYNTHESIS; ESCHERICHIA COLI; IC 50; MINIMUM INHIBITORY CONCENTRATION; NONHUMAN; PSEUDOMONAS AERUGINOSA; SIMULATION; STAPHYLOCOCCUS AUREUS;

3-OXOACYL-(ACYL-CARRIER-PROTEIN) SYNTHASE; ANTI-BACTERIAL AGENTS; BACILLUS SUBTILIS; BINDING SITES; DRUG DESIGN; ESCHERICHIA COLI; ESCHERICHIA COLI PROTEINS; MICROBIAL SENSITIVITY TESTS; MOLECULAR DOCKING SIMULATION; PROTEIN STRUCTURE, TERTIARY; PSEUDOMONAS AERUGINOSA; STAPHYLOCOCCUS AUREUS; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES;

BACILLUS SUBTILIS; BACTERIA (MICROORGANISMS); ESCHERICHIA COLI; NEGIBACTERIA; POSIBACTERIA; PSEUDOMONAS AERUGINOSA; STAPHYLOCOCCUS AUREUS;

EID: 84879416230     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.05.006     Document Type: Article

References (19)

1. M. Leeb Nature 431 2004 892
2. A.C. Price, K.H. Choi, R.J. Heath, Z. Li, S.W. White, and C.O. Rock J. Biol. Chem. 276 2000 6551
3. S.S. Khandekar, D.R. Gentry, G.S. VanAller, P. Warren, H. Xiang, C. Silverman, M.L. Doyle, A.K. Konstantinidis, M. Brandt, R.A. Daines, and J.T. Lonsdale J. Biol. Chem. 274 2001 30025
4. X. Qiu, C.A. Janson, W.W. Smith, M. Head, J. Lonsdale, and A.K. Konstantinidis J. Mol. Biol. 307 2001 343
5. S.S. Khandekar, R.A. Daines, and J.T. Lonsdale Curr. Protein Pept. Sci. 4 2003 21
6. R.J. Heath, and C.O. Rock J. Biol. Chem. 1996 1833 271
7. Z. Nie, C. Perretta, J. Lu, Y. Su, S. Margosiak, K.S. Gajiwala, J. Cortez, V. Nikulin, K.M. Yager, K. Appelt, and S. Chu J. Med. Chem. 48 2005 1596
8. I. Hutchinson, S.A. Jennings, B.R. Vishnuvajjala, A.D. Westwell, and M.F.G. Stevens J. Med. Chem. 45 2002 744
9. K.D. Hargrave, F.K. Hess, and J.T. Oliver J. Med. Chem. 26 1983 1158
10. W.C. Patt, H.W. Hamilton, M.D. Taylor, M.J. Ryan, D.G. Taylor Jr., C.J.C. Connolly, A.M. Doherty, S.R. Klutchko, I. Sircar, B.A. Steinbaugh, B.L. Batley, C.A. Painchaud, S.T. Rapundalo, B.M. Michniewicz, and S.C.J. Olson J. Med. Chem. 35 1992 2562
11. P.K. Sharma, S.N. Sawnhney, A. Gupta, G.B. Singh, and S. Bani Indian J. Chem. 37B 1998 376
12. J.C. Jaen, L.D. Wise, B.W. Caprathe, H. Tecle, S. Bergmeier, C.C. Humblet, T.G. Heffner, L.T. Meltzner, and T.A. Pugsley J. Med. Chem. 33 1990 311
13. K. Tsuji, and H. Ishikawa Bioorg. Med. Chem. Lett. 4 1994 1601
14. F.W. Bell, A.S. Cantrell, M. Hogberg, S.R. Jaskunas, N.G. Johansson, C.L. Jordon, M.D. Kinnick, P. Lind, J.M. Morin Jr., R. Noreen, B. Oberg, J.A. Palkowitz, C.A. Parrish, P. Pranc, C. Sahlberg, R.J. Ternansky, R.T. Vasileff, L. Vrang, S.J. West, H. Zhang, and X.X. Zhou J. Med. Chem. 38 1995 4929
15. N. Ergenc, G. Capan, N.S. Günay, S. Özkirimli, M. Güngor, S. Özbey, and E. Kendi Arch. Pharm. Pharm. Med. Chem. 332 1999 343
16. J.S. Carter, S. Kramer, J.J. Talley, T. Penning, P. Collins, M.J. Graneto, K. Seibert, C. Koboldt, J. Masferrer, and B. Zweifel Bioorg. Med. Chem. Lett. 9 1999 1171
17. H. Kitagawa, T. Ozawa, S. Takahata, M. Iida, J. Saito, and M. Yamada J. Med. Chem. 50 2007 4710
18. X.L. Qiu, G.D. Li, G.K. Wu, J.W. Zhu, L. Zhou, P.L. Chen, A.R. Chamberlin, and W.H. Lee J. Med. Chem. 52 2009 1758
19. G.M. Morris, D.S. Goodsell, R.S. Halliday, R. Huey, W.E. Hart, R.K. Belew, and A.J. Olson J. Comput. Chem. 19 1998 1660