Rational design, synthesis and in vitro characterization of novel potent inhibitors of Pseudomonas aeruginosa multivirulence factor regulator (MvfR)

MvfR in P. aeruginosa is responsible for the expression of many virulence factors and small molecules, including HHQ, PQS and PYO (PYO). PQS, HHQ and PYO are produced both in vitro and in vivo and provide a surrogate measurement to MvfR inhibition.

A discovery program was initiated to discover novel, potent inhibitors of MvfR regulon, starting from a chemical series firstly reported by L Rahme. Here we describe the design and the in vitro characterization of a novel chemical series of MvfR inhibitors designed from M64 taken as the prototype molecule.

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Aptuit | Rational design, synthesis and in vitro characterization of novel potent inhibitors

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