Pyridylpiperazine-based allosteric inhibitors of RND-type multidrug efflux pumps.

C, Plé; HK, Tam; Da Cruz A, Vieira; N, Compagne; JC, Jiménez-Castellanos; RT, Müller; E, Pradel; WE, Foong; G, Malloci; A, Ballée; MA, Kirchner; P, Moshfegh; A, Herledan; A, Herrmann; B, Deprez; N, Willand; AV, Vargiu; KM, Pos; M, Flipo; RC, Hartkoorn

doi:10.1038/s41467-021-27726-2

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Pyridylpiperazine-based allosteric inhibitors of RND-type multidrug efflux pumps.

Shared by NobleBlocks on Jan 10, 2022 • 12:00 AM UTC

Authors:

Plé C

Tam HK

Vieira Da Cruz A

Abstract

Efflux transporters of the RND family confer resistance to multiple antibiotics in Gram-negative bacteria. Here, we identify and chemically optimize pyridylpiperazine-based compounds that potentiate antibiotic activity in E. coli through inhibition of its primary RND transporter, AcrAB-TolC. Charact...

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