Monodisperse oligoethylene glycols modified Propofol prodrugs. Issue 22 (1st December 2018)

• Record Type: Journal Article
• Authors: Deng, Tao; Mao, Xianglan; Li, Yu; Bo, Shaowei; Yang, Zhigang; Jiang, Zhong-Xing
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 28:Issue 22(2018)
• Page Start: 3502
• Page End: 3505
• Publication Date: 2018-12-01
• Subjects: Propofol -- Prodrug -- Polyethylene glycols -- Anesthetic -- Monodisperse; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2018.10.009
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Monodisperse oligoethylene glycol was employed to concisely manipulate the water solubility and anesthetic effects of Propofol, an anesthetics with poor solubility and side effects. Highlights: Prodrugs to overcome major drawbacks of existing drug. Monodisperse PEGs modified drugs. Improved water solubility and comparable drug efficacy. From synthesis, to physicochemical study, to cell and animal study. Abstract: The low water solubility of Propofol resulted in complicated formulation and adverse effects during its clinical application. To improve its water solubility and maintain its anesthetic effects, Propofol prodrugs with monodisperse oligoethylene glycols as solubility enhancer were designed and synthesized. Monodisperse oligoethylene glycols enable the concise manipulation of water solubility, biocompatibility and anesthetic effects. Through the physicochemical and biological assay, a few water soluble prodrugs of Propofol were identified as promising anesthetic to overcome the drawbacks associated with Propofol.