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.

Autor: Eya'ane Meva, Francois, Prior, Timothy J., Evans, David J., Shah, Sachin, Tamngwa, Cynthia Fake, Belengue, Herschelle Guyenne Lagrange, Mang, Roland Emmanuel, Munro, Justin, Qahash, Tarrick, Llinás, Manuel
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Zdroj: Research on Chemical Intermediates; Feb2022, Vol. 48 Issue 2, p885-898, 14p
Abstrakt: 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. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index
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