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Design, synthesis and biological evaluation of α-substituted isonipecotic acid benzothiazole analogues as potent bacterial type II topoisomerase inhibitors.

By Lloyd Czaplewski, Nov 20 2013 07:15PM

Chemical Biology Study points to novel antibacterials

Axford LC, Agarwal PK, Anderson KH, Andrau LN, Atherall J, Barker S, Bennett JM, Blair M, Collins I, Czaplewski LG, Davies DT, Gannon CT, Kumar D, Lancett P, Logan A, Lunniss CJ, Mitchell DR, Offermann DA, Palmer JT, Palmer N, Pitt GR, Pommier S, Price D, Narasinga Rao B, Saxena R, Shukla T, Singh AK, Singh M, Srivastava A, Steele C, Stokes NR, Thomaides-Brears HB, Tyndall EM, Watson D, Haydon DJ.

Bioorg Med Chem Lett. 2013 Nov 4. pii: S0960-894X(13)01264-X. doi: 10.1016/j.bmcl.2013.10.058. [Epub ahead of print]

The discovery and optimisation of a new class of benzothiazole small molecules that inhibit bacterial DNA gyrase and topoisomerase IV are described. Antibacterial properties have been demonstrated by activity against DNA gyrase ATPase and potent activity against Staphylococcus aureus, Enterococcus faecalis, Streptococcus pyogenes and Haemophilus influenzae. Further refinements to the scaffold designed to enhance drug-likeness included analogues bearing an α-substituent to the carboxylic acid group, resulting in excellent solubility and favourable pharmacokinetic properties.



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