Structure Anti-inflammatory Activity Relationship and Biochemical Evaluation of Some Novel Triazoloquinazoline and Triazinoquinazoline Derivatives Containing Sulfacetamide Moiety
نویسنده
چکیده
Department of Biochemistry, Faculty of Pharmacy, October 6th University, October 6th city, Egypt E-mail : [email protected] ABSTRACT-: This study was carried out to evaluate the structure activity relationship and biochemical effects of some novel of anti-inflammatory triazoloquinazolines and triazinoquinazolines containing sulfacetamide moiety. Some of the newly synthesized compounds 4-17 showed good anti-inflammatory activities. Also, the median lethal doses (LD50s) of compounds 8, 10 and 17 in mice were 370, 338 and 295 mg/100g b.w., respectively. Oral administration of compounds 8, 10 and 17 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 and 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, 10 and 17 exhibited good anti-inflammatory activity and more safe on rat liver enzymes.
منابع مشابه
Synthesis and pharmacophore modeling of novel quinazolines bearing a biologically active sulfonamide moiety.
In the present work, interaction of the strategic starting material, methyl 2-isothiocyanatobenzoate (1), with sulfa drugs resulted in the formation of methyl 2-[3-(4-(N-substituted sulfamoyl)phenyl)thioureido] benzoates 2-5, which upon reaction with hydrazine hydrate afforded N-amino derivatives 6-9. Triazoloquinazoline derivatives 10-18 were obtained via reaction of compounds 6-8 with aromati...
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