Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 54, Issue 9, Pages 3418-3425Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm2002124
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We investigated compounds related to the previously reported anti-staphyloccocal 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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