Target-oriented synthesis of antiparasitic 2-hetaryl substituted quinolines based on imino Diels-Alder reactions

被引：32

作者：

Kouznetsov, Vladimir V. ^{[1
]}

Vargas Mendez, Leonor Y.

Milena Leal, Sandra

Mora Cruz, Uriel

Andres Coronado, Carlos

Melendez Gomez, Carlos M.

Romero Bohorquez, Arnold R.

Escobar Rivero, Patricia

机构：

[1] Univ Ind Santander, Escuela Quim, CIBIMOL, Lab Quim Organ & Biomol, Bucaramanga 678 AA, Colombia

[2] Univ Ind Santander, Escuela Med, Dept Ciencias Basicas, CINTROP,Ctr Invest Enfermedades Trop, Bucaramanga 678 AA, Colombia

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2007年 / 4卷 / 04期

关键词：

antiparasitic activities; target-oriented synthesis; 2-hetarylquinolines; Leishmania chagasi; trypanosoma cruzi; drug discovery;

D O I：

10.2174/157018007784620031

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Target-oriented synthesis of new substituted 2-hetarylquinolines 6-19 and their in vitro activity against endemic parasites such as Leishmania chagasi and Trypanosoma cruzi are reported. In addition, their cytotoxicities for mammalian Vero cells and THP-1 macrophages cells are assessed. These studies showed that between the new (tetrahydro)quinolines series tested in these assays, the 4-methyl-8-isopropyl-2-(3-pyridinyl)quinoline 15 exhibits the best in vitro response against both live forms of T. cruzi and L. chagasi parasites and displays no cytotoxic activity on mammalian cells.

引用

页码：293 / 296

页数：4

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