Synthesis of 4-substituted pyrido[2,3- d]pyrimidin-4(1 H)-one as analgesic and anti-inflammatory agents
4-Substituted-pyrido[2,3- d]pyrimidin-4(1 H)-ones 4a– c were synthesized by oxidation of 4-substituted-dihydropyrido[2,3- d]pyrimidin-4(1 H)-ones 3a– c which were in turn prepared from arylidenemalononitriles 1a– c and 6-aminothiouracil 2. The reactivity of compounds 4a– c towards some reagents such...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2009-07, Vol.19 (13), p.3392-3397 |
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Hauptverfasser: | , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | 4-Substituted-pyrido[2,3-
d]pyrimidin-4(1
H)-ones
4a–
c were synthesized by oxidation of 4-substituted-dihydropyrido[2,3-
d]pyrimidin-4(1
H)-ones
3a–
c which were in turn prepared from arylidenemalononitriles
1a–
c and 6-aminothiouracil
2. The reactivity of compounds
4a–
c towards some reagents such as formamide, carbon disulfide, urea, thiourea, formic and acetic acids were studied. All the synthesized compounds were characterized by spectroscopic means and elemental analysis. Compound
4c exhibited 64% and 72% analgesic activity. Also, compound
4b showed 50% and 65% anti-inflammatory activity. Interestingly these compounds showed one-third of ulcer index of the reference aspirin and diclofenac. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2009.05.044 |