European Journal of Medicinal Chemistry p. 4807 - 4812 (2010)
Update date:2022-08-03
Topics:
Sun, Xian-Yu
Hu, Chuan
Deng, Xian-Qing
Wei, Cheng-Xi
Sun, Zhi-Gang
Quan, Zhe-Shan
Starting from phthalic anhydride, several new 6-alkoxy(phenoxy)-[1,2,4] triazolo[3,4-a]phthalazine-3-amine derivatives were synthesized as potent anti-inflammatory agent. The study showed that the compounds 6h (6-(2-chlorophenoxy)-[1,2,4]triazolo[3,4-a]phthalazine-3-amine) and 6s (6-(4-aminophenoxy)-[1,2,4] triazolo[3,4-a]phthalazine-3-amine) exhibited the highest anti-inflammatory activity (81% and 83% inhibition, respectively, at 0.5 h after i.p. administration) which were slightly more potent than the reference drug Ibuprofen (61%). Furthermore, the peak activity of 6h and 6s was observed at the 3 h after p.o. administration, and they exhibited stronger anti-inflammatory activity than Ibuprofen at the dose of 50 mg/kg at the peak time.
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