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Microwave assisted green chemistry approach to the synthesis of some novel N1-amino-methyl-substituted 1,4-Benzodiazepine derivatives

机译:微波辅助绿色化学方法合成一些新型的N1-氨基-甲基取代的1,4-苯并二氮杂卓衍生物

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An efficient microwave assisted protocol for the exclusive one pot synthesis of N-amino-methyl substituted 1,4- benzodiazepine derivatives 4(a-f) and 5(a-f) by the reaction of N-amino-methyl substituted isatoic anhydride 1(a-f) with glycine and L-proline respectively has been described. Treatment of N-amino-methyl substituted isatoic anhydride 1(a-f) with amino acids glycine and L-proline afforded 4(a-f) and 5(a-f) respectively in excellent yield. The derivatives of N-aminomethyl substituted 1,4-benzodiazepine 4(a-f) and 5(a-f) were screened for their in-vitro antimicrobial activities against bacterial species (E.coli and B.subtilis) and fungal species (A.niger and A.flavus) by Agar-well assay method against the standard drugs (ciprofloxacin for bacteria and fluconazol for fungi).
机译:通过N-氨基-甲基取代的等角酸酐1(af)与N-氨基-甲基取代的1,4-苯并二氮杂derivatives衍生物4(af)和5(af)的唯一一锅合成的高效微波辅助规程已经分别描述了甘氨酸和L-脯氨酸。用氨基酸甘氨酸和L-脯氨酸处理N-氨基甲基取代的等角酸酐1(a-f),分别以优异的收率得到4(a-f)和5(a-f)。筛选了N-氨基甲基取代的1,4-苯并二氮杂卓4(af)和5(af)的衍生物对细菌菌种(E.coli和B.subtilis)和真菌菌种(A.niger和A.niger)的体外抗菌活性。用Agar-well分析法对标准药物(细菌用环丙沙星和真菌用氟康唑)进行黄曲霉。

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