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Synthesis and biological evaluation of 1-amino isochromans from 2-bromoethyl benzaldehyde and amines in acid medium
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2017-11-14 , DOI: 10.1016/j.bmcl.2017.11.020
Narjis Fatima , B.V. Subba Reddy , Sabitha Gowravaram , J.S. Yadav , Sudhakar Kadari , Chandra Shekar Putta

We have developed a facile and efficient synthetic route to substituted isochromans for the first time by reacting 2-(2-bromoethyl)benzaldehyde with a variety of aryl, heteroaryl amines in AcOH. The reaction is catalyst/additive free and takes place at reflux conditions with short reaction time to furnish products in good to excellent yields. All the compounds have been characterized by spectral techniques such as IR, 1H NMR and Mass etc. Synthesized compounds were evaluated for antimicrobial activity against specific bacterial like 1) Staphylococcus strains aureus 2) Bacillus subtilis 3) Escherichia coli 4) Pseudomonas aeruginosa. Compounds 3e, 3n, 3 m, 3 l, 3 k, 3j and 3b showed most potent in vitro activity against bacterial strains.



中文翻译:

在酸性介质中由2-溴乙基苯甲醛和胺合成1-氨基异色团并进行生物评价

我们首次通过使2-(2-溴乙基)苯甲醛与AcOH中的各种芳基,杂芳基胺反应,首次开发了一种简便有效的合成取代异色满的方法。该反应不含催化剂/添加剂,并且在回流条件下以短的反应时间进行,从而以良好至优异的产率提供产物。所有的化合物的特点是光谱技术如IR,1 H NMR和质谱等合成的化合物进行了评价针对特定细菌样1的抗微生物活性)菌株金黄色葡萄球菌2)枯草芽孢杆菌3)大肠埃希氏菌4)铜绿假单胞菌。化合物3e,3n,3 m,3 l,3 k,3j3b3b显示了对细菌菌株的最有效的体外活性。

更新日期:2017-11-14
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