4.5 Article

Synthesis and antinociceptive activity of pyrazolyl isoxazolines and pyrazolyl isoxazoles

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 13, Pages 3370-3373

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.05.055

Keywords

1,3-Dipolar cycloaddition; Pyrazolyl isoxazoline; Pyrazolyl isoxazole; Antinociceptive activity

Funding

  1. Council of Scientific and Industrial Research, New Delhi, India

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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. (C) 2009 Elsevier Ltd. All rights reserved.

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