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Phosphate-Based Self-Immolative Linkers for the Delivery of Amine-Containing Drugs

M. Đud, M. Tichotová, E. Procházková, O. Baszczyňski

. 2021 ; 26 (17) : . [pub] 20210825

Jazyk angličtina Země Švýcarsko

Typ dokumentu časopisecké články

Perzistentní odkaz   https://www.medvik.cz/link/bmc21025090

Grantová podpora
20-25137Y Grantová Agentura České Republiky
21-23014S Grantová Agentura České Republiky
SG-2018-1 Nadace Experientia

Amine-containing drugs often show poor pharmacological properties, but these disadvantages can be overcome by using a prodrug approach involving self-immolative linkers. Accordingly, we designed l-lactate linkers as ideal candidates for amine delivery. Furthermore, we designed linkers bearing two different cargos (aniline and phenol) for preferential amine cargo release within 15 min. Since the linkers carrying secondary amine cargo showed high stability at physiological pH, we used our strategy to prepare phosphate-based prodrugs of the antibiotic Ciprofloxacin. Therefore, our study will facilitate the rational design of new and more effective drug delivery systems for amine-containing drugs.

Citace poskytuje Crossref.org

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