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Taylor & Francis Journals Auto-Holdings Collection
Beschreibungen/Notizen
Development of dual-acting antibacterial agents containing Erlotinib, a recognized EGFR inhibitor used as an anticancer agent, with differently spaced benzenesulfonamide moieties known to bind and inhibit
carbonic anhydrase (
CA) or the antiviral Zidovudine.
Through rational design, ten derivatives were obtained via a straightforward synthesis including a click chemistry reaction. Inhibitory activity against a panel of pathogenic carbonic anhydrases and antibacterial susceptibility of
ATCC 43504 were assessed. Docking studies on α-carbonic anhydrase enzymes and EGFR were conducted to gain insight into the binding mode of these compounds.
Some compounds proved to be strong inhibitors of
CA and showed good anti-
activity. Computational studies on the targeted enzymes shed light on the interaction hotspots.