(1R, 2R, 6S)-3-methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol derivatives as promising compounds for anti-Parkinsonian activity

Parkinson’s disease is a progressive neurodegenerative disorder characterized by tremors, bradykinesia, rigidity and postural instability. Levodopa, the main drug for Parkinson’s disease treatment, has serious side effects. For that reason, exploring medical drug for new effective treatment is extremely important. Recently, in Novosibirsk Institute of Organic Chemistry it was found that monoterpenoid (1R, 2R, 6S)-3-methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol (1) demonstrated high anti-Parkinsonian activity in vivo on MPTP models in mice and rats.

In the current work, several modifications of compound 1 at different sites were carried out. Although most modifications led to decrease in activity, a few new compounds demonstrated promising anti-Parkinsonian activity.

Research showed that inserting in (1R, 2R, 6S)-3-methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol substituents like propylthio and butyl increased the activity. Derivatives of (1S, 5S, 6R)-2-methyl-5-(prop-1-en-2-yl)-7 oxabicyclo[4.1.0]hept-2-ene were also studied.

Acknowledgements: This work was supported by RFBR Grant 19-03-00071