2. Academic Validation
  3. Selenophene-containing inhibitors of type IIA bacterial topoisomerases

Selenophene-containing inhibitors of type IIA bacterial topoisomerases

  • J Med Chem. 2011 May 12;54(9):3418-25. doi: 10.1021/jm2002124.
Jason A Wiles 1,  Avinash S Phadke,  Barton J Bradbury,  Michael J Pucci,  Jane A Thanassi,  Milind Deshpande
Affiliations

Affiliation

  • 1 Achillion Pharmaceuticals, Inc., 300 George Street, New Haven, Connecticut 06511, United States. jwiles@achillion.com
PMID: 21443219 DOI: 10.1021/jm2002124
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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