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- Title
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.
- Authors
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
- 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.
- Subjects
ETHYL esters; DRUG synthesis; ASPIRIN; NUCLEAR magnetic resonance spectroscopy; OXALYL chloride; INFRARED spectroscopy; ELEMENTAL analysis
- Publication
Research on Chemical Intermediates, 2022, Vol 48, Issue 2, p885
- ISSN
0922-6168
- Publication type
Article
- DOI
10.1007/s11164-021-04607-3