Synthetic Transformations of Higher Terpenoids. 45#. Regioselective Synthesis of 5-Labdanoid-Substituted Pyrazoles and Assessment of Their Analgesic Activity
M. E. Mironov, A. I. Poltanovich, V. I. Krasnov, T. V. Rybalova, S. A. Borisov, T. G. Tolstikova, E. E. Shults
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引用次数: 0
Abstract
A method for targeted structural modification of the methyl ester of phlomisoic acid was developed by introduction of an additional C-16 ketopyrazole moiety via cyclocondensation of diterpenoid alkyne-1,2- diones with arylhydrazines. The conditions for regioselective formation of labdanoid 1,3-diarylpyrazol-5- ylmethanones were found. The possibility of a sequential four-component reaction in a single pot was demonstrated. Significant analgesic activity of labdanoid-substituted diarylpyrazoles in thermal and chemical irritation models was established.
期刊介绍：
Chemistry of Natural Compounds publishes reviews and general articles about the structure of different classes of natural compounds, the chemical characteristics of botanical families, genus, and species, to establish the comparative laws and connection between physiological activity and the structure of substances.
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