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Synthesis and anti-inflammatory activity of certain piperazinylthienylpyridazine derivatives

  • Hanan M. RefaatEmail author
  • Omneya M. Khalil
  • Hanan H. Kadry
Article Drug discovery

Abstract

In this study, a novel series of 2-(4-substituted piperazin-l-ylmethyl)-6-(thien-2-yl)-2H-pyridazin-3-ones(3a- f), 2-(4-substituted piperazin-l-yl carbonylmethyl)-6-(thien-2-yl)-2H-pyridazin-3-ones(4a- c) and 2-[2-(4-substituted piperazin-l-ylcarbonylethyl)]-6-(thien-2-yl)-2H-pyridazin-3-ones(5a,b) were prepared from 6-(thien-2-yl)-2H- pyridazin-3-one(1). In addition, 3-(4-substituted piperazin-l-ylcarbonyl methyl thio)-6-(thien-2-yl) pyridazines(6a- c) and 3-[2-(4-substitutedpiperazin-l-ylcarbonyl ethylthio]-6-(thien-2-yl) pyridazines(7a,b) were synthesized. Furthermore, 5-(4-substituted piperazin-l-ylmethyl)-6-(thien-2-yl)-2H-pyridazin-3-ones(12a,b) were prepared. The structures of the new compounds were confirmed by elemental analysis as well as by1H-NMR,IR andMS data. Some of the newly prepared compounds were subjected to evaluation for their anti-inflammatory activity against carrageenan-induced paw edema at a dose of 10 mg/kg using indomethacin as the reference standard.

Key words

Piperazinylthienylpyridazinones S-Piperazinylpyridazines Anti-inflammatory activity 

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Copyright information

© The Pharmaceutical Society of Korea 2007

Authors and Affiliations

  • Hanan M. Refaat
    • 1
    Email author
  • Omneya M. Khalil
    • 1
  • Hanan H. Kadry
    • 1
  1. 1.Organic Chemistry DepartmentFaculty of Pharmacy, Cairo UniversityCairoEgypt

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