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.

• MeSH
• aminy chemie   MeSH
• antibakteriální látky chemie   MeSH
• ciprofloxacin chemie   MeSH
• fosfáty chemie   MeSH
• koncentrace vodíkových iontů MeSH
• kyselina mléčná chemie   MeSH
• léčivé přípravky chemie   MeSH
• prekurzory léčiv chemie   MeSH
• systémy cílené aplikace léků metody   MeSH
• Publikační typ
• časopisecké články MeSH