Synthesis and antitubercular activity of substituted phenylmethyl- and pyridylmethyl amines
Synthesis and antitubercular activity of substituted phenylmethyl- and pyridylmethyl amines
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DOI：
10.1016/j.bmc.2006.09.020
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发表时间：
2006-12-15
影响因子：
3.5
通讯作者：
Sinha, S.
中科院分区：
文献类型：
--
作者：
Tripathi, R. P.;Saxena, Nisha;Sinha, S.
通过芳香/杂芳醛与胺的还原胺化或通过胺与肉桂酸酯的共轭加成，然后用锂铝、氢化物将酯基还原为各自的丙醇胺，合成了42个苄基甲基胺和吡啶甲基胺。所有合成的化合物对结核分枝杆菌的无毒株和强毒株均有抑制作用。许多化合物的最低抑菌浓度为1.56微克/毫升。几乎没有有效的化合物对耐多药结核病的临床分离株进行了评估，发现它们在一个或另一个浓度下具有活性，最低抑菌浓度为3.12微克/毫升。(C)2006爱思唯尔有限公司。保留所有权利。
A total of 42 benzyl- and pyridylmethyl amines were synthesized either by reductive amination of aromatic/heteroaromatic aldehydes with amines or by conjugate addition of amines to the cinnamates followed by reduction of the ester group with lithium aluminium, hydride to the respective propanolamines. All the synthesized compounds were evaluated against both avirulent and virulent strains of Mycobacterium tuberculosis. Many of the compounds exhibited MIC as low as 1.56 mu g/mL. Few of potent compounds were also evaluated against clinical isolates of MDR TB and found to be active at one or other concentrations with MIC as low as 3.12 mu g/mL. (c) 2006 Elsevier Ltd. All rights reserved.