Journal of Medicinal Chemistry p. 5157 - 5168 (2014)
Update date:2022-08-04
Topics:
Sp?th, Andreas
Leibl, Christoph
Cieplik, Fabian
Lehner, Karin
Regensburger, Johannes
Hiller, Karl-Anton
B?umler, Wolfgang
Schmalz, Gottfried
Maisch, Tim
Increasing antibiotic resistances in microorganisms create serious problems in public health. This demands alternative approaches for killing pathogens to supplement standard treatment methods. Photodynamic inactivation of bacteria (PIB) uses light activated photosensitizers (PS) to generate reactive oxygen species immediately upon illumination, inducing lethal phototoxicity. Positively charged phenalen-1-one derivatives are a new generation of PS for light-mediated killing of pathogens with outstanding singlet oxygen quantum yield ΦΔ of >97%. Upon irradiation with a standard photopolymerizer light (bluephase C8, 1260 ± 50 mW/cm2) the PS showed high activity against the oral key pathogens Enterococcus faecalis, Actinomyces naeslundii, Streptococcus mutans, and Aggregatibacter actinomycetemcomitans. At a concentration of 10 μM, a maximum efficacy of more than 6 log10 steps (≥99.9999%) of bacteria killing is reached in less than 1 min (light dose 50 J/cm2) after one single treatment. The pyridinium substituent as positively charged moiety is especially advantageous for antimicrobial action.
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