Journal
BIOORGANIC CHEMISTRY
Volume 97, Issue -, Pages -Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2020.103661
Keywords
Antimicrobial resistance; Photodynamic therapy; Porphycene; Singlet oxygen; Photosensitizer conjugates; Amphiphilicity
Funding
- Spanish Ministerio de Economia y Competitividad [CTQ2016-78454-C2-1-R]
- SUR del DEC de la Generalitat de Catalunya [2017 FI_B_00617, 2018 FI_B1 00174, 2019 FI_B2 00167]
- FSE [2017 FI_B_00617, 2018 FI_B1 00174, 2019 FI_B2 00167]
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A novel photoantimicrobial agent, namely 2-aminothiazolo [4,5-c]-2,7,12,17-tetrakis(methoxyethyl)porphycene (ATAZTMPo-gentamicin) conjugate, has been prepared by a click reaction between the red-light absorbing 9-isothiocyanate-2,7,12,17-tetrakis(methoxyethyl)porphycene (9-ITMPo) and the antibiotic gentamicin. The conjugate exhibits submicromolar activity in vitro against both Gram-positive and Gram-negative bacteria (Staphylococcus aureus and Escherichia coli, respectively) upon exposure to red light and is devoid of any cytotoxicity in the dark. The conjugate outperforms the two components delivered separately, which may be used to enhance the therapeutic index of gentamicin, broaden the spectrum of pathogens against which it is effective and reduce its side effects. Additionally, we report a novel straightforward synthesis of 2,7,12,17-tetrakis(methoxyethyl) porphycene (TMPo) that decreases the number of steps from nine to six.
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