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Photoactivatable Heptamethine-Based Carbonic Anhydrase Inhibitors Leading to New Anti-Antibacterial Agents.

Authors :
Carradori, Simone
Angeli, Andrea
Sfragano, Patrick S.
Yzeiri, Xheila
Calamante, Massimo
Tanini, Damiano
Capperucci, Antonella
Kunstek, Hannah
Varbanov, Mihayl
Capasso, Clemente
Supuran, Claudiu T.
Source :
International Journal of Molecular Sciences; Jun2023, Vol. 24 Issue 11, p9610, 12p
Publication Year :
2023

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. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
16616596
Volume :
24
Issue :
11
Database :
Complementary Index
Journal :
International Journal of Molecular Sciences
Publication Type :
Academic Journal
Accession number :
164218526
Full Text :
https://doi.org/10.3390/ijms24119610