PEG-amino acid-przewaquinone a conjugations: Synthesis, physicochemical properties and protective effect in a rat model of brain ischemia-reperfusion.

Authors :: Wang M
Niu A
Gong Z
Xu Z
Li L
Li B
Wang J
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2020 Jan 01; Vol. 30 (1), pp. 126780. Date of Electronic Publication: 2019 Oct 31.
Publication Year :: 2020
Abstract: A total of 21 PEG-przewaquinone A conjugations with high drug loading ability, good water solubility and in vivo slow-release quality were obtained by conjugating przewaquinone A with PEG through amino acids and tripeptides spacers respectively. Notably, compound 3a can obviously reduce the brain ischemia-reperfusion damage dose-dependently in a rat model, which indicated the efficacy of our PEG prodrug strategy.<br /> (Copyright © 2019. Published by Elsevier Ltd.)

Subjects :: Animals
Brain Ischemia pathology
Disease Models, Animal
Diterpenes pharmacology
Male
Quinones pharmacology
Rats
Rats, Sprague-Dawley
Reperfusion Injury pathology
Brain Ischemia drug therapy
Diterpenes therapeutic use
Quinones therapeutic use
Reperfusion Injury drug therapy

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