a Gram-negative bacterium ― is involved in the most serious stomach pathologies, including gastric ulcer and cancer. One of the most effective and widely used drugs against H. pylori is the macrolide clarithromycin (CLM). Unfortunately, CLM can inhibit the human ether-à-go-go-related gene (hERG) channel, associated with long QT syndrome (LQTS) liability. The aim of this work was to develop novel compounds with off-target activities on cardiac sodium channels (Nav 1.5) and calcium channels (Cav 1.2) (CUPID).
Mexiletine-Derived (Thio)Ureas as Modulators of both Antimicrobial Activity and Cardiac Liability of Clarithromycin
L. Quintieri;W. Schirinzi;L. Caputo;
2025
Abstract
a Gram-negative bacterium ― is involved in the most serious stomach pathologies, including gastric ulcer and cancer. One of the most effective and widely used drugs against H. pylori is the macrolide clarithromycin (CLM). Unfortunately, CLM can inhibit the human ether-à-go-go-related gene (hERG) channel, associated with long QT syndrome (LQTS) liability. The aim of this work was to develop novel compounds with off-target activities on cardiac sodium channels (Nav 1.5) and calcium channels (Cav 1.2) (CUPID).File in questo prodotto:
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