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Updated: Jun 3, 2026

Simple and Fast Rolling Circle Amplification-Based Detection of Topoisomerase 1 Activity in Crude Biological Samples
Published on: December 2, 2022
Selenophene-containing inhibitors of type IIA bacterial topoisomerases
Jason A Wiles1, Avinash S Phadke, Barton J Bradbury
1Achillion Pharmaceuticals, Inc., 300 George Street, New Haven, Connecticut 06511, United States. jwiles@achillion.com
Abstract:
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.
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