Antimycobacterial activity generated by the amide coupling of (-)-fenchone derived aminoalcohol with cinnamic acids and analogues

被引：14

作者：

Slavchev, Ivaylo ^{[1
]}

Dobrikov, Georgi M. ^{[1
]}

Valcheva, Violeta ^{[2
]}

Ugrinova, Iva ^{[3
]}

Pasheva, Evdokia ^{[3
]}

Dimitrov, Vladimir ^{[1
]}

机构：

[1] Bulgarian Acad Sci, Ctr Phytochem, Inst Organ Chem, Sofia 1113, Bulgaria

[2] Bulgarian Acad Sci, Stephan Angeloff Inst Microbiol, Sofia 1113, Bulgaria

[3] Bulgarian Acad Sci, Inst Mol Biol Roumen Tsanev, Sofia 1113, Bulgaria

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 21期

关键词：

Fenchone; Amides; Cinnamic acids; Tuberculosis; DRUG SENSITIVITY; TUBERCULOSIS; OPTIMIZATION; GROWTH;

D O I：

10.1016/j.bmcl.2014.09.021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Aminoethyl substituted 2-endo-fenchol prepared from (-)-fenchone was used as scaffold for the synthesis of series of 31 amide structures by N-acylation applying cinnamic acids and analogues. The evaluation of their in vitro activity against Mycobacterium tuberculosis H(37)Rv showed for some of them promising activity-up to 0.2 mu g/ml, combined with relatively low cytotoxicity of the selected active compounds. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：5030 / 5033

页数：4

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