Anti-inflammation and antimalarial profile of 5-pyridin-2-yl-1H-[1,2,4]triazole-3-carboxylic acid ethyl ester as a low molecular intermediate for hybrid drug synthesis

被引：0
|
作者：
Francois Eya’ane Meva
Timothy J. Prior
David J. Evans
Sachin Shah
Cynthia Fake Tamngwa
Herschelle Guyenne Lagrange Belengue
Roland Emmanuel Mang
Justin Munro
Tarrick Qahash
Manuel Llinás
机构：
[1] University of Douala,Department of Pharmaceutical Sciences, Faculty of Medicine and Pharmaceutical Sciences
[2] University of Hull,Department of Chemistry and Biochemistry
[3] The Pennsylvania State University,Department of Biochemistry and Molecular Biology
[4] University of Douala,Department of Chemistry
[5] The Pennsylvania State University,Department of Chemistry
[6] The Pennsylvania State University,Huck Center for Malaria Research
[7] John Innes Centre,undefined
[8] Norwich Research Park,undefined
来源：
Research on Chemical Intermediates | 2022年 / 48卷
关键词：
1.2.4-triazole; Synthesis; Structure; Anti-inflammation; Antimalarial;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
A novel 1,2,4-triazole intermediate 5-pyridin-2-yl-1H-[1,2,4]triazole-3-carboxylic acid ethyl ester was prepared by the reaction of N’-aminopiridyne-2-carboximidamine and an excess monoethyl oxalyl chloride and screened for biological activities. The compound was structurally characterized by nuclear magnetic resonance spectroscopy, elemental analysis, infrared spectroscopy, and single-crystal X-ray diffraction. Bioassays indicated that the compound exhibits potent anti-inflammation activity in vitro. An egg albumin denaturation assay to assess the anti-inflammatory effect of the synthesized compound showed a significant inhibition of protein with a maximum inhibition of 71.1% at the highest tested concentration (1000 µg/mL) compared to 81.3% for Aspirin as standard drug. The antimalarial activity on the 3D7 P. falciparum strain was determined to be IC50 176 µM and was obtained prior to connection with pharmacophoric groups.
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页码：885 / 898
页数：13
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