Details

Autor(en) / Beteiligte

• Velema, Willem A
• Hansen, Mickel J
• Lerch, Michael M
• Driessen, Arnold J. M
• Szymanski, Wiktor
• Feringa, Ben L

Titel

Ciprofloxacin–Photoswitch Conjugates: A Facile Strategy for Photopharmacology

Ist Teil von

• Bioconjugate chemistry, 2015-12, Vol.26 (12), p.2592-2597

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2015

Quelle

MEDLINE

Beschreibungen/Notizen

• 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.