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.
Keywords: Synthesis, heterocyclic compounds, anti-inflammatory, triazole, indomethacin, ear-edema test.
Letters in Drug Design & Discovery
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.
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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
DOI https://dx.doi.org/10.2174/1570180812666150630184439 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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