Erlotinib-Containing Benzenesulfonamides As Anti- <i>Helicobacter Pylori</i> Agents Through Carbonic Anhydrase Inhibition

Abstract

<b>Aim:</b> 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 <i>Helicobacter pylori</i> carbonic anhydrase (<i>Hp</i>CA) or the antiviral Zidovudine. <b>Methods & materials:</b> 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 <i>H. pylori</i> 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. <b>Results & conclusion:</b> Some compounds proved to be strong inhibitors of <i>Hp</i>CA and showed good anti-<i>H. pylori</i> activity. Computational studies on the targeted enzymes shed light on the interaction hotspots.