Français
Albanian
Arabic
Armenian
Azerbaijani
Belarusian
Bengali
Bosnian
Catalan
Czech
Danish
Deutsch
Dutch
English
Estonian
Finnish
Français
Greek
Haitian Creole
Hebrew
Hindi
Hungarian
Icelandic
Indonesian
Irish
Italian
Japanese
Korean
Latvian
Lithuanian
Macedonian
Mongolian
Norwegian
Persian
Polish
Portuguese
Romanian
Russian
Serbian
Slovak
Slovenian
Spanish
Swahili
Swedish
Turkish
Ukrainian
Vietnamese
Български
中文(简体)
中文(繁體)
Current Topics in Medicinal Chemistry 2017

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

Seuls les utilisateurs enregistrés peuvent traduire des articles
Se connecter S'inscrire
Le lien est enregistré dans le presse-papiers
Michel Lapier
Maria C Zuniga-Lopez
Benjamin Aguilera-Venegas
Rosa Adam
Belen Abarca
Rafael Ballesteros
Rodrigo Lopez-Munoz
Juan Diego Maya
Claudio Olea-Azar

Mots clés

Abstrait

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.

RESULTS

Our results showed that the series is capable of generating a stable radical species and generate ROS in the parasite. On the other hand these molecules are potent inhibitors of enzymes belonging to the complex P450. We have focused on the inhibition of ergosterol biosynthesis demonstrating that triazole/ pyridine families are able to affect this pathway being observed the accumulation of squalene and lanosterol.

Rejoignez notre
page facebook

La base de données d'herbes médicinales la plus complète soutenue par la science

  • Fonctionne en 55 langues
  • Cures à base de plantes soutenues par la science
  • Reconnaissance des herbes par image
  • Carte GPS interactive - étiquetez les herbes sur place (à venir)
  • Lisez les publications scientifiques liées à votre recherche
  • Rechercher les herbes médicinales par leurs effets
  • Organisez vos intérêts et restez à jour avec les nouvelles recherches, essais cliniques et brevets

Tapez un symptôme ou une maladie et lisez des informations sur les herbes qui pourraient aider, tapez une herbe et voyez les maladies et symptômes contre lesquels elle est utilisée.
* Toutes les informations sont basées sur des recherches scientifiques publiées

Google Play badgeApp Store badge