Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, Part 2
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- 作者：Wilson Cunico ; Claudia R.B. Gomes ; Victor Facchinetti ; Marcele Moreth ; Carmen Penido ; Maria G.M.O. Henriques ; Fern ; o P. Varotti ; Luisa G. Krettli ; Antoniana U. Krettli ; Franklin S. da Silva ; Ernesto R. Caffarena ; Camila S. de Magalhã ; es
- 关键词：Protease inhibitor ; Malaria ; Hydroxyethylamine
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2009
- 出版时间：September 2009
- 年：2009
- 卷：44
- 期：9
- 页码：3816-3820
- 全文大小：273 K
文摘
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.