Oleg V. Ardashov

Highly potent activity of (1R,2R,6S)-3-methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol in animal models of Parkinson's disease.

(1R,2R,6S)-3-Methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol 1 possesses potent antiparkinsonian activity in both MPTP and haloperidol animal models. The use of compound 1 resulted in nearly full recovery of the locomotor and exploratory activities and was as effective as the comparator agent (levodopa). All eight stereoisomers of compound 1 have been synthesized and the influence of the absolute configuration on the antiparkinsonian activity of compound 1 was shown.

Selective Preparation of trans-Carveol over Ceria Supported Mesoporous Materials MCM-41 and SBA-15

Ce-modified mesoporous silica materials MCM-41 and SBA-15, namely 32 wt % Ce–Si–MCM-41, 16 wt % Ce–H–MCM-41 and 20 wt % Ce–Si–SBA-15, were prepared, characterized and studied in the selective preparation of trans-carveol by α-pinene oxide isomerization. The characterizations of these catalysts were performed using scanning electron microscopy, X-ray photoelectron spectroscopy, nitrogen adsorption and FTIR pyridine adsorption. Selective preparation of trans-carveol was carried out in the liquid phase in a batch reactor. The activity and the selectivity of catalyst were observed to be influenced by their acidity, basicity and morphology of the mesoporous materials. The formation of trans-carveol is moreover strongly influenced by the basicity of the used solvent and in order to achieve high yields of this desired alcohol it is necessary to use polar basic solvent.

Antiviral Activity of 3-methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol and its Derivatives Against Influenza A(H1N1)2009 Virus

A number of new derivatives of monoterpenoid with a para-menthane framework 3-methyl-6-(prop-1-en-2- yl)cyclohex-3-ene-1,2-diol (-)-3 were synthesized. The antiviral activity of (-)-3 and its derivatives against the pandemic influenza virus A/California/07/09 (H1N1)v was studied in vitro. Compound (-)-3 was found to be active against this vi- rus (selectivity index 7.5); for mononicotinate (+)-6 the selectivity index was 17. The absolute configuration of compound 6 was shown to be critical for its antiviral activity.

3-Methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol: the Importance of Functional Groups for Antiparkinsonian Activity

Compounds with different sets of three of the four functional groups of (1R,2R,6S)-3-methyl-6-(prop-1-en-2- yl)cyclohex-3-ene-1,2-diol 1 possessing high antiparkinsonian activity were synthesized. The synthesized compounds were tested for the antiparkinsonian activity in vivo on a mouse model with MPTP neurotoxin. A pronounced antiparkinsonian effect of 1 can only be achieved if it contains all the four functional groups (two hydroxy groups and two double bonds). The 2-hydroxy group or the 3,4-double bond is not required for stimulating the exploratory activity of the animals.

Unusual products of the reactions of verbenone and verbenol with N-bromosuccinimide in the presence of water

The major products of the reactions of (−)-verbenone and (+)-trans-verbenol with N-bromosuccinimide in the presence of water were compounds having an oxabicyclo[3.2.1]octane skeleton but containing different numbers of bromine atoms in their molecules.

The action of monoterpenoids with promising antiparkinsonian activity on fertility of Drosophila melanogaster

Adequate treatment of Parkinson’s disease is an important medical issue. Patients are suffered from numerous side effects of the widely used drugs. It has been found recently that monoterpenoid (1R,2R,6S)-3-methyl-6-(prop-1-en-2-yl) cyclohex-3-ene-1,2-diol and its diacetate demonstrate high antiparkinsonian activity in some animal models. At the same time, their genetic safety was not studied yet. The aim of this research was to investigate the effect of these compounds with antiparkinsonian activities on reproduction of D. melanogaster. Over 4000 of fruitflies cultivated under the action of these compounds were analyzed. It was found that the chemicals did not provoke genetic mutations or alter reproduction of D. melanogaster. The possible explanations for the detected phenomena are provided. It was found that the compounds do not affect fertility in Drosophila..