Synthesis and biological evaluation against Mycobacterium tuberculosis and Leishmania amazonensis of a series of diaminated terpenoids

被引：7

作者：

dos Reis, Dijovani Batista ^{[1
]}

Alves Souza, Thalita Cristina ^{[1
]}

Lourenco, Maria Cristina S. ^{[2
]}

de Almeida, Mauro Vieira ^{[3
]}

Barbosa, Adriano ^{[4
]}

Eger, Iriane ^{[4
]}

Saraiva, Mauricio Frota ^{[1
]}

机构：

[1] Univ Fed Itajuba, Inst Fis & Quim, BR-37500903 Itajuba, MG, Brazil

[2] Fundacao Oswaldo Cruz, Dept Bacteriol, Inst Pesquisas Clin Evandro Chagas, Av Brasil 4365, Manguinho, RJ, Brazil

[3] Univ Fed Juiz de Fora, Inst Ciencias Exatas, Dept Quim, BR-36036330 Juiz De Fora, MG, Brazil

[4] Univ Estadual Ponta Grossa, Dept Biol Geral, Av Gen Carlos Cavalcanti 4746, Ponta Grossa, PR, Brazil

来源：

BIOMEDICINE & PHARMACOTHERAPY | 2016年 / 84卷

关键词：

Tuberculosis; Leishmaniasis; Diamine; Terpenoid; ALAMAR BLUE ASSAY; ANTILEISHMANIAL ACTIVITY; IN-VITRO; TRYPANOCIDAL ACTIVITIES; SUSCEPTIBILITY; DERIVATIVES;

D O I：

10.1016/j.biopha.2016.10.112

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

We report the synthesis of a series of diaminated terpenoids containing, as side-chain of the diamine core, the "head-to-tail" prenyl derivatives, with amino amino spacers of variable length. In vitro biological activity of these compounds was evaluated against Mycobacterium tuberculosis and Leishmania amazonensis, and the structure-activity relationships are discussed. Different biological results were observed depending on the terpenic side-chain length. The best results were obtained for trans, trans-farnesol derivatives. Moreover, these results demonstrated that the stereochemistry of the double bond could play an important role in determining antitubercular and antileishmanial activities of these compounds. (C) 2016 Elsevier Masson SAS. All rights reserved.

引用

页码：1739 / 1747

页数：9

共 18 条

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