1440-78-4Relevant academic research and scientific papers
Design, Synthesis, and Activity Study of Water-Soluble, Rapid-Release Propofol Prodrugs
Liu, Liang-Quan,Hong, Pei-Xi,Song, Xing-Hai,Zhou, Chang-Cui,Ling, Rui,Kang, Yi,Qi, Qing-Rong,Yang, Jun
, p. 7857 - 7866 (2020)
In this work, a series of water-soluble propofol prodrugs were synthesized, and their propofol release rate and pharmacodynamic characteristics were measured. We found that inserting glycolic acid as a linker between propofol and the cyclic amino acid accelerated the release of propofol from prodrugs into the plasma while preserving its safety. In animal experiments, prodrugs (3e, 3g, and 3j) were significantly better than fospropofol (the only water-soluble propofol prodrug that has been used clinically) in terms of safety, onset, and duration time of anesthesia. Their molar dose, onset time, and anesthesia duration time were comparable to those of propofol, helping to maintain the clinical benefits of propofol. The experimental results showed the potential of such compounds as water-soluble prodrugs of propofol.
Substituted phenol hydroxy acid ester N-containing derivative as well as preparation and application thereof
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Paragraph 0042-0044, (2021/04/26)
The invention provides a substituted phenol hydroxy acid ester N-containing derivative as well as preparation and application thereof. The compound is shown as a formula (I). The salt of the compound in the formula (I) has good water solubility, can rapid
