Synthesis of some novel triazoloquinazolines and triazinoquinazolines and their evaluation for anti-inflammatory activity

A series of triazoloquinazolines and triazinoquinazolines were synthesized as novel anti-inflammatory agents. Some of the newly synthesized compounds 8 , 11 , and 19 showed good anti-inflammatory activities. Also, the median lethal doses (LD 50s ) of compounds 8 , 11 , and 19 in mice were 222.25, 21...

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Veröffentlicht in:Medicinal chemistry research 2012-08, Vol.21 (8), p.1876-1886
1. Verfasser: Hussein, Mohammed Abdalla
Format: Artikel
Sprache:eng
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Zusammenfassung:A series of triazoloquinazolines and triazinoquinazolines were synthesized as novel anti-inflammatory agents. Some of the newly synthesized compounds 8 , 11 , and 19 showed good anti-inflammatory activities. Also, the median lethal doses (LD 50s ) of compounds 8 , 11 , and 19 in mice were 222.25, 213.25, and 235 mg/100 g b.w., respectively. Oral administration of compounds 8 , 11 , and 19 to the rats at dose of 300 mg/kg b.w. for 10 days showed non-significant changes in liver enzymes SGOT, SGPT, ALP, LDH, γ-GT, SOD, GPx, and blood GSH and serum TBARs as compared with the control group. But, administration of indomethacin orally to the rats at a concentration of 600 mg/kg b.w. daily for 10 days to rats showed significant increase in serum SGOT, SGPT, ALP, LDH, γ-GT, and TBARs and significant decrease in blood GSH, SOD, and GPx. These findings suggest that compounds 8 , 11 , and 19 exhibited good anti-inflammatory activity and more safe on liver enzymes in rats.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-011-9707-0