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Structure-activity relationships of novel tryptamine-based inhibitors of bacterial transglycosylase
Sosič, Izidor ...
Penicillin-binding proteins represent well-established, validated and still very promising targets for the design and development of new antibacterial agents. The transglycosylase domain of ...penicillin-binding proteins is especially important, as it catalyzes polymerization of glycan chains, using the peptidoglycan precursor lipid II as a substrate. Based on the previous discovery of a non-covalent small-molecule inhibitor of transglycosylase activity, we systematically explored the structure-activity relationships of these tryptamine-based inhibitors. The main aim was to reduce the non-specificcytotoxic properties of the initial hit compound, and concurrentlyto retain the mode of its inhibition. A focused library of tryptamine-based compounds was synthesized, characterized, and evaluated biochemically. The results presented here show the successful reduction of thenon-specific cytotoxicity, and the retention of the inhibition of transglycosylase enzymatic activity, as well as the ability of these compounds to bind to lipid II and to have antibacterial actions.
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