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Sep 2019 ACS infectious diseases

Cyclipostins and Cyclophostin Analogues as Multitarget Inhibitors That Impair Growth of .


Madani A, Ridenour JN, Martin BP, Paudel RR, Abdul Basir A, Le Moigne V, Herrmann JL, Audebert S, Camoin L, Kremer L, Spilling CD, Canaan S, Cavalier JF


Twelve new Cyclophostin and Cyclipostins analogues () were synthesized, thus extending our series to 38 . Their antibacterial activities were evaluated against four pathogenic mycobacteria (, , BCG, and ) and two Gram negative bacteria. The displayed very low toxicity toward host cells and were only active against mycobacteria. Importantly, several were active against extracellular (///) or intramacrophage residing mycobacteria (/) with minimal inhibitory concentrations (MIC) values comparable to or better than those of amikacin or imipenem, respectively. An activity-based protein profiling combined with mass spectrometry allowed identification of the potential target enzymes of /, mostly being involved in lipid metabolism and/or in cell wall biosynthesis. Overall, these results strengthen the selective activity of the against mycobacteria, including the most drug-resistant , through the cumulative inhibition of a large number of Ser- and Cys-enzymes participating in key physiological processes.

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