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
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
Authors
Francois Eya’ane Meva
Dr Tim Prior T.Prior@hull.ac.uk
Senior Lecturer in Inorganic Chemistry
David J. Evans
Sachin Shah
Cynthia Fake Tamngwa
Herschelle Guyenne Lagrange Belengue
Roland Emmanuel Mang
Justin Munro
Tarrick Qahash
Manuel Llinás
Abstract
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.
Citation
Eya’ane Meva, F., Prior, T. J., Evans, D. J., Shah, S., Tamngwa, C. F., Belengue, H. G. L., Mang, R. E., Munro, J., Qahash, T., & Llinás, M. (2022). 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. Research on Chemical Intermediates, 48(2), 885–898. https://doi.org/10.1007/s11164-021-04607-3
