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

Title: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

Volume: 13 Issue: 2

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Pan Fu-Jun, Wang Shi-Ben, Liu Da-Chuan, Gong Guo-Hua and Quan Zhe-Shan, 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, Letters in Drug Design & Discovery 2016; 13(2) . https://dx.doi.org/10.2174/1570180812666150630184439