Abstract: Earlier it was found, that (1R,2R,6S)-3-methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol (1) possess high antiparkinsonian activity. The N-, O-, S- and C-derivatives at the C-9 position of diol 1 were synthesized in this work. The antiparkinsonian activity of these compounds was studied in MPTP mice models. As a rule, the introduction of substituents containing nitrogen atoms at the C-9 position led to a considerable decrease or loss of antiparkinsonian activity. A derivative of 2-aminoadamantane 8 significantly decreased the locomotor activity time, thus enhancing the symptoms of the parkinsonian syndrome. However the introduction of butyl or propylthio substituents at the C-9 position of diol 1 did not diminish the antiparkinsonian activity comparing to parent compound. This information is important when choosing a route for immobilization of compound 1 to find possible targets. (C) 2013 Elsevier Ltd. All rights reserved.

Cite: Ardashov O.V. , Pavlova A.V. , Korchagina D.V. , Volcho K.P. , Tolstikova T.G. , Salakhutdinov N.F.
Antiparkinsonian activity of some 9-N-, O-, S- and C-derivatives of 3-methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol
Bioorganic and Medicinal Chemistry. 2013. V.21. N5. P.1082-1087. DOI: 10.1016/j.bmc.2013.01.003 WOS Scopus РИНЦ

Dates:

Published print:

Mar 1, 2013

Identifiers:

Web of science	WOS:000314689200006
Scopus	2-s2.0-84873743106
Elibrary	20433729
OpenAlex	W2056014369

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