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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis of 4-Phenylthieno[2,3-e][1,2,4]triazolo[4,3-a]pyrimidine-5(4H)-one Derivatives and Evaluation of Their Anti-inflammatory Activity

Author(s): Fu-Jun Pan, Shi-Ben Wang, Da-Chuan Liu, Guo-Hua Gong and Zhe-Shan Quan

Volume 13, Issue 2, 2016

Page: [141 - 148] Pages: 8

DOI: 10.2174/1570180812666150630184439

Price: $65


A series of 4-phenylthieno[2,3-e][1,2,4]triazolo[4,3-a]pyrimidine-5(4H)-ones (5a–p) with triazole or other heterocyclic substituents (6–11) was synthesized and the compounds were evaluated for their anti-inflammatory activity using the xylene-induced ear-edema test. Pharmacological analyses showed that the compound 4-(4-chlorophenyl)thieno[2,3-e][1,2,4]triazolo[4,3-a]pyrimidine- 5(4H)-one (5m) exhibited the greatest anti-inflammatory activity (50.48% inhibition, 30 min after intraperitoneal administration) and was more potent than the reference drug, indomethacin. The peak activity of 5m was observed 4 h after oral administration, and it showed a higher anti-inflammatory activity than indomethacin did at a dose of 100 mg/kg.

Keywords: Synthesis, heterocyclic compounds, anti-inflammatory, triazole, indomethacin, ear-edema test.

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