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Selenophene-Containing Inhibitors of Type IIA Bacterial Topoisomerases

2011; American Chemical Society; Volume: 54; Issue: 9 Linguagem: Inglês

10.1021/jm2002124

1520-4804

Jason A. Wiles, Avinash Phadke, Barton J. Bradbury, Michael J. Pucci, Jane A. Thanassi, Milind Deshpande,

Synthesis and bioactivity of alkaloids

We investigated compounds related to the previously reported antistaphyloccocal agent AVE6971 in an effort to attenuate inhibition of hERG potassium channel current that has been noted for this and related antibacterial drug classes. While most modifications of the original thiophene group compromised antibacterial activity, one selenophene analogue displayed (i) improved activity against the primary target enzyme DNA gyrase, (ii) similar activities against a panel of MRSA clinical isolates, and (iii) reduced hERG channel inhibition.