期刊
BIOCONJUGATE CHEMISTRY
卷 26, 期 12, 页码 2592-2597出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.bioconjchem.5b00591
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资金
- Netherlands Organization for Scientific Research (NWO) [723.014.001]
- Royal Netherlands Academy of Arts and Sciences Science (KNAW)
- Ministry of Education, Culture and Science [024.001.035]
- European Research Council [227897]
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.
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