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Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2.

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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Cunico W,Gomes CR,Facchinetti V,Moreth M,Penido C,Henriques MG,Varotti FP,Krettli LG,Krettli AU,da Silva FS,Caffarena ER,de Magalhães CS

doi

10.1016/j.ejmech.2009.03.041

subject

Has Abstract

pub_date

2009-09-01 00:00:00

pages

3816-20

issue

9

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(09)00199-8

journal_volume

44

pub_type

杂志文章

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