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Article

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

1
Faculty of Science, Charles University, 128 43 Prague, Czech Republic
2
Institute of Organic Chemistry and Biochemistry, The Czech Academy of Sciences, 166 10 Prague, Czech Republic
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Silvia Arpicco
Molecules 2021, 26(17), 5160; https://doi.org/10.3390/molecules26175160
Received: 23 July 2021 / Revised: 12 August 2021 / Accepted: 20 August 2021 / Published: 25 August 2021
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. View Full-Text
Keywords: 31P-NMR spectroscopy; amine-containing drugs; phosphate-based linkers; prodrugs; self-immolative linkers 31P-NMR spectroscopy; amine-containing drugs; phosphate-based linkers; prodrugs; self-immolative linkers
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MDPI and ACS Style

Đud, M.; Tichotová, M.; Procházková, E.; Baszczyňski, O. Phosphate-Based Self-Immolative Linkers for the Delivery of Amine-Containing Drugs. Molecules 2021, 26, 5160. https://doi.org/10.3390/molecules26175160

AMA Style

Đud M, Tichotová M, Procházková E, Baszczyňski O. Phosphate-Based Self-Immolative Linkers for the Delivery of Amine-Containing Drugs. Molecules. 2021; 26(17):5160. https://doi.org/10.3390/molecules26175160

Chicago/Turabian Style

Đud, Mateja, Markéta Tichotová, Eliška Procházková, and Ondřej Baszczyňski. 2021. "Phosphate-Based Self-Immolative Linkers for the Delivery of Amine-Containing Drugs" Molecules 26, no. 17: 5160. https://doi.org/10.3390/molecules26175160

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