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- W4362608306 abstract "Legionella pneumophila is the causative agent of Legionnaires’ disease, a serious form of pneumonia. Its macrophage infectiv-ity potentiator (Mip), a member of a highly conserved family of FK506-binding proteins, plays a major role in the prolifera-tion of the Gram-negative bacterium in host organisms. In this work, we test our library of >1000 FKBP-focused ligands for inhibition of LpMip. The [4.3.1]-bicyclic sulfonamide turned out as a highly preferred scaffold and provided the most potent LpMip inhibitors known so far. Selected compounds were non-toxic to human cells, displayed antibacterial activity and block bacterial proliferation in cellular infection-assays as well as infectivity in human lung tissue explants. The results confirm [4.3.1]-bicyclic sulfonamides as anti-legionellal agents, although their anti-infective properties cannot be explained by inhibi-tion of LpMip alone." @default.
- W4362608306 created "2023-04-06" @default.
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- W4362608306 date "2023-04-05" @default.
- W4362608306 modified "2023-09-27" @default.
- W4362608306 title "[4.3.1] Bicyclic FKBP ligands inhibit Legionella pneumophila infection by LpMip-dependent and LpMip independent mechanisms" @default.
- W4362608306 doi "https://doi.org/10.26434/chemrxiv-2023-vfssm" @default.
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