Synthesis and Pharmacological Properties of 2-[S-Acetylthiorphan]-l,3-diacylaminopropan-2-ol Derivatives as Chimeric Lipid Drug Carriers Containing an Enkephalinase Inhibitor

@article{Lambert1995SynthesisAP,
  title={Synthesis and Pharmacological Properties of 2-[S-Acetylthiorphan]-l,3-diacylaminopropan-2-ol Derivatives as Chimeric Lipid Drug Carriers Containing an Enkephalinase Inhibitor},
  author={Didier Lambert and Frank Mergen and Catherine F. Berens and Jacques H. Poupaert and Pierre Dumont},
  journal={Pharmaceutical Research},
  year={1995},
  volume={12},
  pages={187-191}
}
The design of 1,3-diacylaminopropan-2-ols as CNS-directed carrier groups is based on their resemblance to endogenous lipids and the properties of pseudotriglyceride esters to facilitate the brain penetration of therapeutic agents. 2-[S-acetylthiorphan]-l,3-diacylaminopropan-2-ols, differing from the nature of 1,3-acyl chains, were synthesized and evaluated in vivo using the hot-plate jump test. The compounds exhibited naloxone reversible analgesic properties. The effects were superior to those… CONTINUE READING