Synthesis and anti-mycobacterial activity of novel amino alcohol derivatives

被引：24

作者：

Cunico, Wilson ^{[1
,3
]}

Gomes, Claudia R. B. ^{[1
]}

Ferreira, Maria L. G. ^{[1
]}

Ferreira, Thais G. ^{[1
]}

Cardinot, Danielle ^{[1
]}

de Souza, Marcus V. N. ^{[1
]}

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

机构：

[1] FioCruz Fundacao Oswaldo Cruz, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, Brazil

[2] FioCruz Fundacao Oswaldo Cruz, Dept Bacteriol, Inst Pesquisas Clin Evandro Chagas, BR-21041250 Rio De Janeiro, Brazil

[3] Univ Fed Pelotas, Dept Quim Organ, NuQuiA Nucleo Quim Aplicada, BR-96010900 Pelotas, RS, Brazil

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 03期

关键词：

Tuberculosis; Amino alcohols; Hydroxyethylamines; ASPARTYL PROTEASE INHIBITORS; ALAMAR BLUE ASSAY; MYCOBACTERIUM-TUBERCULOSIS; ANTIMALARIAL ACTIVITY; PLASMODIUM-FALCIPARUM; D-MANNITOL; SUSCEPTIBILITY; ETHAMBUTOL; FUTURE; DESIGN;

D O I：

10.1016/j.ejmech.2011.01.004

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Thirteen new hydroxyethylamines have been synthesized from reactions of (2S,3S)Boc-phenylalanine epoxide, piperonylamine and arenesulfonyl chlorides in good yields. These compounds were evaluated as antibacterial agents against Mycobacterium tuberculosis H37Rv using the Alamar Blue susceptibility test and their activity expressed as the minimum inhibitory concentration (MIC) in mu M. Two amino alcohols displayed significant activity when compared with first line drug ethambutol (EMB). Therefore this class of compounds could be a good starting point to develop new lead compounds in the treatment of tuberculosis. (C) 2011 Elsevier Masson SAS. All rights reserved.

引用

页码：974 / 978

页数：5

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