207497-42-5Relevant articles and documents
Cerium(IV) mediated oxygenation of dialkyl malonates: A novel synthesis of tartronic acid derivatives
Nair, Vijay,Nair, Latha G.,Mathew, Jessy
, p. 2801 - 2804 (1998)
A novel Cerium(IV) mediated oxygenation of dialkyl malonates leading to a direct synthesis of tartronic acid derivatives is described.
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
supporting information, p. 7857 - 7866 (2020/08/21)
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.
