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区域选择性反应:一些源自1,2,4-三唑的新型曼尼希碱的合成、表征及药理学研究

Regioselective reaction: synthesis, characterization and pharmacological studies of some new Mannich bases derived from 1,2,4-triazoles.

作者信息

Isloor Arun M, Kalluraya Balakrishna, Shetty Prashanth

机构信息

Department of Chemistry, National Institute of Technology-Karnataka, Surathkal, Mangalore 575 025, India.

出版信息

Eur J Med Chem. 2009 Sep;44(9):3784-7. doi: 10.1016/j.ejmech.2009.04.038. Epub 2009 May 5.

Abstract

In the present investigation, a series of new 4[(3-substituted-1H-pyrazol-4-yl)methyleneamino]-5-substituted-2-[(4-methylpiperzine-1-yl)methyl]-2H-1,2,4-triazole-3(4H)-thiones (4) were synthesized by the aminomethylation of 4-(3-substituted-1H-pyrazol-3-yl)methyleneamino-5-substituted-4H-1,2,4-triazole-3-thiols (3) with formaldehyde and N-methylpiperzine. These newly synthesized Schiff and Mannich bases were characterized by IR, (1)H NMR, mass spectral data and elemental analyses. These compounds were screened for their antibacterial and antifungal activity. Some of the compounds were found to exhibit significant antimicrobial activity.

摘要

在本研究中,通过4-(3-取代-1H-吡唑-3-基)亚甲基氨基-5-取代-4H-1,2,4-三唑-3-硫醇(3)与甲醛和N-甲基哌嗪的氨甲基化反应,合成了一系列新的4-[(3-取代-1H-吡唑-4-基)亚甲基氨基]-5-取代-2-[(4-甲基哌嗪-1-基)甲基]-2H-1,2,4-三唑-3(4H)-硫酮(4)。这些新合成的席夫碱和曼尼希碱通过红外光谱、¹H核磁共振、质谱数据和元素分析进行了表征。对这些化合物进行了抗菌和抗真菌活性筛选。发现其中一些化合物具有显著的抗菌活性。

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