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Int J Mol Sci ; 24(11)2023 Jun 01.
Article in English | MEDLINE | ID: mdl-37298561

ABSTRACT

With the aim to propose innovative antimicrobial agents able to not only selectively inhibit bacterial carbonic anhydrases (CAs) but also to be photoactivated by specific wavelengths, new heptamethine-based compounds decorated with a sulfonamide moiety were synthesized by means of different spacers. The compounds displayed potent CA inhibition and a slight preference for bacterial isoforms. Furthermore, minimal inhibitory and bactericidal concentrations and the cytotoxicity of the compounds were assessed, thus highlighting a promising effect under irradiation against S. epidermidis. The hemolysis activity test showed that these derivatives were not cytotoxic to human red blood cells, further corroborating their favorable selectivity index. This approach led to the discovery of a valuable scaffold for further investigations.


Subject(s)
Antineoplastic Agents , Carbonic Anhydrases , Humans , Structure-Activity Relationship , Carbonic Anhydrase Inhibitors/pharmacology , Carbonic Anhydrases/metabolism , Antineoplastic Agents/pharmacology , Anti-Bacterial Agents/pharmacology , Carbonic Anhydrase IX/metabolism , Molecular Structure
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