Synthesis of limonene β-amino alcohol derivatives in support of new antileishmanial therapies

被引：16

作者：

Ferrarini, Stela R. ^{[1
]}

Graebin, Cedric S. ^{[1
]}

Limberger, Jones ^{[2
]}

Canto, Romulo F. S. ^{[1
]}

Dias, Daiane O. ^{[1
]}

da Rosa, Ricardo G. ^{[2
]}

Madeira, Maria de Fatima ^{[3
]}

Eifler-Lima, Vera L. ^{[1
]}

机构：

[1] Univ Fed Rio Grande do Sul, Lab Sintese Organ Med, BR-90610000 Porto Alegre, RS, Brazil

[2] Univ Fed Rio Grande do Sul, Lab Catalise Metais Transicao, BR-90610000 Porto Alegre, RS, Brazil

[3] Fiocruz MS, Serv Parasitol Clin, Inst Pesquisa Clin Evandro Chagas, BR-21045900 Rio De Janeiro, Brazil

来源：

MEMORIAS DO INSTITUTO OSWALDO CRUZ | 2008年 / 103卷 / 08期

关键词：

limonene; beta-amino alcohol; synthesis; leishmaniasis; Leishmania braziliensis; neglected diseases;

D O I：

10.1590/S0074-02762008000800005

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：

A series of seven limonene beta-amino alcohol derivatives has been regioselectively synthesised in moderate to good yields. Two of these compounds were found to be significantly effective against in vitro cultures of the Leishmania (Viannia) braziliensis promastigote form in the micromolar range. The activities found for 3b and 3f were about 100-fold more potent than the standard drug, Pentamidine, in the same test, while limonene did not display any activity. This is the first report of antileishmanial activity by limonene beta-amino alcohol derivatives.

引用

页码：773 / 777

页数：5

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