Nesterkina M. Novel derivatives of terpenoids with anticonvulsant, analgesic and anti-inflammatory activity

Esters based on mono-/bicyclic terpenoids with neurotransmitter amino acids ? gamma-aminobutyric acid (GABA) and glycine were synthesized for this purpose. Chemical synthesis, physico-chemical methods: 1H NMR spectroscopy, mass spectrometry, IR- and UV-spectroscopy, fluorescence analysis, X-ray analysis, TLC, pharmacological methods: acute toxicity, analgesic, anti-inflammatory and anticonvulsant activity. The mechanism of action for synthesized terpenoid esters with GABA on phospholipids of artificial membranes and lipids isolated from the stratum corneum of experimental animals has been studied. Acute toxicity (LD50) after oral and intravenous administration was investigated. In the study of antiseizure activity the obtained esters were found to exhibit anticonvulsant action in a time range from 1 to 24 hours after oral administration. The presence of analgesic and anti-inflammatory effect of synthesized terpenoid esters after their transdermal delivery was defined. The mechanism of combined esters action associated with their interaction with TRP, GABA and glycine receptor was suggested. Scope - bioorganic chemistry.