Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 41, Issue 2, Pages 155-165Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2005.09.006
Keywords
ethyl arylidenecyanoacetate; arylidenemalononitrile; ethoxymethylene-2-phenyl-2-oxazolin-5-one; dimethyl acetonedicarboxylate; 1-(imidazol-2-yl and pyrimidin-2-yl)-3-pyrazolin-5-ones synthesis; 2-(imidazol-2-yl and pyrimidin-2-yl)-1,2,4,5,6,7-hexahydro-3H-indazol-3-ones synthesis; antiinflammatory activity; analgesic activity; antipyretic activity; NSAIDs
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As a part of a research project on the synthesis of a number of substituted 1-(pyrimidin-2-yl)-3-pyrazolin-5-ones and 2-(pyrimidin-2-yl)hexahydroindazol-3-ones and as a result of the interesting anti inflammatory, analgesic and antipyretic activities recorded for some of these compounds, some new 3-pyrazolin-5-ones and hexahydroindazol-3-ones linked to substituted imidazolyl, pyrimidyl and tetrahydroquinazolinyl moieties were prepared and evaluated for such activity (Fig. 1). A structure-activity relationship (SAR) comparative study indicated that some compounds from 3-pyrazolin-5-one (2, 6-8, 10) and indazolone (18, 20, 24, 27, 29) series exhibited pronounced anti inflammatory, analgesic and antipyretic activities relative to indomethacin. Most of these compounds were found to be nearly equipotent in the anti inflammatory screen (ED50 = 16.8-19.9 mg/kg) whereas the lead compound, 2-indazolyi-4-pyrimidineacetic acid 24 (Fig. 1), was found to be the most potent among this series (ED50 = 9-9 mg/kg). Additionally, the most active compounds were shown to have a large safety margin (ALD(50) = 3.0 g/kg, po) and devoid of ulcerogenic potentialities when administered orally at a dose of 300 mg/kg. (c) 2005 Elsevier SAS. All rights reserved.
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