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Ciprofloxacin-Photoswitch Conjugates: A Facile Strategy for Photopharmacology

Velema, W. A., Hansen, M. J., Lerch, M. M., Driessen, A. J. M., Szymanski, W. & Feringa, B. L., Dec-2015, In : BIOCONJUGATE CHEMISTRY. 26, 12, p. 2592-2597 6 p.

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  • Ciprofloxacin-Photoswitch Conjugates A Facile Strategy for Photopharmacology

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DOI

Photopharmacology aims to locally treat diseases and study biological processes with photoresponsive drugs. Herein, easy access to photoswitchable drugs is crucial, which is supported by simple and robust drug modifications. We investigated the possibility of creating drugs that can undergo remote activation and deactivation with light, by conjugating molecular photoswitches to the exterior of an existing drug in a single chemical step. This facile strategy allows the convenient introduction of various photochromic systems into a drug molecule, rendering it photoresponsive. To demonstrate the feasibility of this approach, two photoswitch-modified ciprofloxacin antibiotics were synthesized. Remarkably, for one of them a 50-fold increase in activity compared to the original ciprofloxacin was observed. Their antimicrobial activity could be spatiotemporally controlled with light, which was exemplified by bacterial patterning studies.

Original languageEnglish
Pages (from-to)2592-2597
Number of pages6
JournalBIOCONJUGATE CHEMISTRY
Volume26
Issue number12
Publication statusPublished - Dec-2015

    Keywords

  • AZOBENZENE PHOTOSWITCHES, OPTICAL CONTROL, ESCHERICHIA-COLI, VISIBLE-LIGHT, BLIND MICE, IN-VIVO, INHIBITORS, RECEPTORS, SWITCHES, PROTEIN

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