Synthesis and antibacterial activity of some new 1-heteroaryl-5-amino-3H/methyl-4-phenylpyrazoles
Synthesis and antibacterial activity of some new 1-heteroaryl-5-amino-3H/methyl-4-phenylpyrazoles
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DOI：
10.1016/j.bmc.2005.10.026
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发表时间：
2006-03-15
影响因子：
3.5
通讯作者：
Singh, SP
中科院分区：
文献类型：
--
作者：
Aggarwal, R;Kumar, V;Singh, SP
1-杂芳基-5-氨基-4-苯基吡唑3a-g和1-杂芳基-5-氨基-3-甲基-4-苯基吡唑3 h-n的区域选择性合成通过分别用α-苯基甲酰基乙腈2a和α-苯基乙酰基乙腈2b处理杂芳基肼la-g来实现。化合物3的结构由H-1和C-13 NMR谱确定。所有的14个化合物进行了测试，其在体外抗菌活性对三个革兰氏阳性菌和两个革兰氏阴性菌。其中6个化合物3a、3d、3e、3g、31和3 n与市售抗生素（利奈唑胺和头孢肟酯）的药效相当或更强。(c)2005爱思唯尔有限公司保留所有权利。
The regioselective synthesis of 1-heteroaryl-5-amino-4-phenylpyrazoles 3a-g and I -heteroaryl-5-amino-3-methyl-4-phenylpyrazoles 3h-n was achieved by the treatment of heteroarylhydrazines la-g with alpha-phenylforniylacetonitrile 2a and alpha-phenylacetylacetonitrile 2b, respectively. The structures of the compounds 3 were established by the combined use of H-1 and C-13 NMR spectroscopy. All the fourteen compounds were tested for their in vitro antibacterial activity against three Gram-positive and two Gram-negative bacteria. Six compounds 3a, 3d, 3e, 3g, 31, and 3n frorn this series were found to be equipotent or more potent than the commercial antibiotics (Linezolid and Cefroxime axetil). (c) 2005 Elsevier Ltd. All rights reserved.