Microwave assisted synthesis of novel pyrazolone derivatives attached to a pyrimidine moiety and evaluation of their anti-inflammatory, analgesic and antipyretic activities
In the present research work, the motto was to develop new chemical entities as potential anti-inflammatory, analgesic and antipyretic agents. Various 4-(2-amino-6-(substituted)pyrimidin-4-yl)-3-methyl-1-(substituted)-1 H-pyrazol-5(4 H)-one derivatives ( 5a– 5j) and their Schiff bases ( 6a– 6j) were...
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Veröffentlicht in: | Saudi pharmaceutical journal 2011-10, Vol.19 (4), p.233-243 |
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Hauptverfasser: | , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | In the present research work, the motto was to develop new chemical entities as potential anti-inflammatory, analgesic and antipyretic agents. Various 4-(2-amino-6-(substituted)pyrimidin-4-yl)-3-methyl-1-(substituted)-1
H-pyrazol-5(4
H)-one derivatives (
5a–
5j) and their Schiff bases (
6a–
6j) were synthesized. The newly synthesized compounds were characterized by TLC and spectral data. The compounds containing pyrazolone and amino pyrimidine as basic moieties (
5a–
5j), were screened for their anti-inflammatory, analgesic and antipyretic activities, compounds
5a,
5c–
5f,
5h exhibited activities nearly similar to the standard. The pharmacological studies reveal that the presence of 4-hydroxy, 4-methoxy, 4-(N,N-dimethylamino) or 2-hydroxy groups on phenyl ring at C
6 of amino pyrimidine exhibits anti-inflammatory, analgesic and antipyretic activities nearly similar to the standard and substitutions like 4-chloro, 2-nitro, 3-nitro or 4-nitro on same phenyl ring lead to a decrease in activities. |
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ISSN: | 1319-0164 2213-7475 |
DOI: | 10.1016/j.jsps.2011.05.006 |