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...
Gespeichert in:
Veröffentlicht in: | Medicinal chemistry research 2012-08, Vol.21 (8), p.1876-1886 |
---|---|
1. Verfasser: | |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
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 |