Related Experiment Video
Updated: May 16, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Synthesis of 5-oxyquinoline derivatives for reversal of multidrug resistance
Torsten Dittrich1, Nils Hanekop, Nacera Infed
1Institute of Organic and Macromolecular Chemistry, University of Düsseldorf, Universitätsstr. 1, D-40225 Düsseldorf, Germany.
Abstract:
The inhibition of ABC (ATP binding cassette) transporters is considered a powerful tool to reverse multidrug resistance. Zosuquidar featuring a difluorocyclopropyl-annulated dibenzosuberyl moiety has been found to be an inhibitor of the P-glycoprotein, one of the best-studied multidrug efflux pumps. Twelve 5-oxyisoquinoline derivatives, which are analogues of zosuquidar wherein the dibenzosuberyl-piperazine moiety is replaced by either a diarylaminopiperidine or a piperidone-derived acetal or thioacetal group, have been synthesized as pure enantiomers. Their inhibitory power has been evaluated for the bacterial multidrug-resistance ABC transporter LmrCD and fungal Pdr5. Four of the newly synthesized compounds reduced the transport activity to a higher degree than zosuquidar, being up to fourfold more efficient than the lead compound in the case of LmrCD and about two times better for Pdr5.
Related Concept Videos
Inhibitors of Bacterial DNA Synthesis
Treatment Resistant Cancers
Combined Effects of Drugs: Synergism
Such synergistic combinations...
Oxidation of Phenols to Quinones
o-hydroxy phenols are oxidized to o-quinones and p-hydroxy phenols to p-quinones. Such redox reactions involve the transfer of two electrons and two protons. The reversible redox property is crucial in...
Radical Chain-Growth Polymerization: Overview
Pharmaceutical Poisoning: Treatment Strategies

