Erlotinib-containing benzenesulfonamides as anti- Helicobacter pylori agents through carbonic anhydrase inhibition

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.