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Improved Potency of Indole-Based NorA Efflux Pump Inhibitors: From Serendipity toward Rational Design and Development

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journal contribution
posted on 02.12.2016, 00:00 by Federica Buonerba, Susan Lepri, Laura Goracci, Bryan D. Schindler, Susan M. Seo, Glenn W. Kaatz, Gabriele Cruciani
The NorA efflux pump is a potential drug target for reversal of resistance to selected antibacterial agents, and recently we described indole-based inhibitor candidates. Herein we report a second class of inhibitors derived from them but with significant differences in shape and size. In particular, compounds 13 and 14 are very potent inhibitors in that they demonstrated the lowest IC50 values (2 μM) ever observed among all indole-based compounds we have evaluated.