Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2.
Eur J Med Chem
; 44(9): 3816-20, 2009 Sep.
Article
de En
| MEDLINE
| ID: mdl-19403210
ABSTRACT
The antimalarial acitivity of hydroxyethylamines, synthesized from the reaction of intermediated hydroxyethypiperazines with benzenesulfonyl chlorides or benzoyl chlorides, has been evaluated in vitro against a W2 Plasmodium falciparum clone. Some of the nineteen tested derivatives showed a significant activity in vitro, thus turning into a promising new class of antimalarials. In addition, a molecular modeling study of the most active derivative (5l) was performed and its most probable binding modes within plasmepsin II enzyme were identified.
Texte intégral:
1
Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Plasmodium falciparum
/
Paludisme à Plasmodium falciparum
/
Éthanolamines
/
Antipaludiques
Limites:
Animals
/
Humans
Langue:
En
Journal:
Eur J Med Chem
Année:
2009
Type de document:
Article
Pays d'affiliation:
Brésil