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

doi:10.2174/1570180812666150630184439

Paper

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

Published Nov 12, 2015 · Fusheng Pan, Shiben Wang, Dachuan Liu

Letters in Drug Design & Discovery

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11

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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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Study Snapshot

The compound 4-(4-chlorophenyl)thieno[2,3-e][1,2,4]triazolo[4,3-a]pyrimidine-5(4H)-one (5m) demonstrates the greatest anti-inflammatory activity, with a higher potency than indometh

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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

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