Synthesis and antinociceptive activity of pyrazolyl isoxazolines and pyrazolyl isoxazoles

Bioorganic & Medicinal Chemistry Letters
2009.0

Abstract

Pyrazolyl isoxazolines and isoxazoles were synthesised in moderate to good yields using 1,3-dipolar cycloaddition of pyrazole derived nitrile oxide with various dipolarophiles such as N-substituted maleimide, diethylacetylene dicarboxylate and phenylacetylene. The synthesized compounds were evaluated for antinociceptive activities. The 3-pyrazolyl-4,5-dicarbethoxy isoxazoles (9a-c) exhibited the maximum antinociceptive activity.

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