Anti-Trypanosoma cruzi and anti-leishmanial activity by quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives

被引：46

作者：

Carlos Villalobos-Rocha, Juan ^{[1
]}

Sanchez-Torres, Luvia ^{[2
]}

Nogueda-Torres, Benjamin ^{[1
]}

Segura-Cabrera, Aldo ^{[3
]}

Garcia-Perez, Carlos A. ^{[3
]}

Bocanegra-Garcia, Virgilio ^{[3
]}

Palos, Isidro ^{[4
]}

Monge, Antonio ^{[5
]}

Rivera, Gildardo ^{[3
]}

机构：

[1] Inst Politecn Nacl, Escuela Nacl Ciencias Biol, Dept Parasitol, Mexico City 11340, DF, Mexico

[2] Inst Politecn Nacl, Escuela Nacl Ciencias Biol, Dept Inmunol, Mexico City 11340, DF, Mexico

[3] Inst Politecn Nacl, Ctr Biotecnol Genom, Esq Elias Pina 88710, Reynosa, Mexico

[4] Univ Autonoma Tamaulipas, Dept Quim Aplicada, Reynosa 88740, Mexico

[5] Univ Navarra, Ctr Invest Farmacobiol Aplicada, Unidad Invest & Desarrollo Medicamentos, Pamplona 31008, Spain

来源：

PARASITOLOGY RESEARCH | 2014年 / 113卷 / 06期

关键词：

Biological activity; Leishmania mexicana; Molecular docking; Quinoxaline 1,4-di-N-oxide; Trypanosoma cruzi; Trypanothione reductase; IN-VITRO; QUINOXALINE 1,4-DI-N-OXIDE; TRYPANOTHIONE REDUCTASE; SULFONAMIDE DERIVATIVES; CHAGAS-DISEASE; VISUALIZATION; DISCOVERY; DOCKING; UPDATE; AGENTS;

D O I：

10.1007/s00436-014-3850-8

中图分类号：

R38 [医学寄生虫学]; Q [生物科学];

学科分类号：

07 ; 0710 ; 09 ; 100103 ;

摘要：

In this work, a novel series of ethyl and methyl quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives were evaluated in vitro on Trypanosoma cruzi trypomastigotes and Leishmania mexicana promastigotes, and cytotoxicity activity in murine macrophages was tested. In silico molecular docking simulations of trypanothione reductase were also done. Three compounds of 33 quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives showed better anti-T. cruzi activity than nifurtimox and beznidazole; two compounds had better anti-leishmanial activity that amphotericin-B, and two compounds showed better activity against both parasites than reference drugs. Compounds M2, M7, M8 and E5, showed low cytotoxic activity on the host cell. The in silico studies suggest that compound M2 is a potential trypanothione reductase inhibitor.

引用

页码：2027 / 2035

页数：9

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