Evaluation of the Novel Antichagasic Activity of [1,2,3]Triazolo[1,5-a]pyridine Derivatives

Title:Evaluation of the Novel Antichagasic Activity of [1,2,3]Triazolo[1,5-a]pyridine Derivatives

Volume: 17 Issue: 4

Author(s): Michel Lapier, Maria C. Zuniga-Lopez, Benjamin Aguilera-Venegas, Rosa Adam, Belen Abarca, Rafael Ballesteros, Rodrigo Lopez-Munoz, Juan Diego Maya and Claudio Olea-Azar

Affiliation:

Keywords: Triazole/Pyridine derivatives, Trypanosoma cruzi, Reactive oxygen species, CYP51, Sterol pathways, Mass spectrometry.

Abstract: Background: Trypanosoma cruzi is the causative agent of Chagas disease. This parasite is vulnerable to the effects of ROS as its main defense mechanism against exogenous agents trypanothione is also another weakness of the parasite that investigated related to the inhibition of enzymes belonging P450 system, mainly CYP51. In our group we have synthesized a series of triazoles known as [1,2,3]triazolo[1,5-a]pyridyl ketones, and pyridyl ketones. These families have shown interesting structural features due to the presence of electron withdrawing moieties attached to the main heterocycle (triazoles and/or pyridines) and are proposed as potential target in the parasite, by the presence of the carbonyl group being able to be reduced and form a free radical that could interact with molecular oxygen generating ROS in the parasite. Furthermore, the triazole ring and pyridines have been considered as potent inhibitors of sterol biosynthesis, the lock being part CYP51.

Cite this article as:

Lapier Michel, Zuniga-Lopez C. Maria, Aguilera-Venegas Benjamin, Adam Rosa, Abarca Belen, Ballesteros Rafael, Lopez-Munoz Rodrigo, Maya Diego Juan and Olea-Azar Claudio, Evaluation of the Novel Antichagasic Activity of [1,2,3]Triazolo[1,5-a]pyridine Derivatives, Current Topics in Medicinal Chemistry 2017; 17 (4) . https://dx.doi.org/10.2174/1568026616666160824103040