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新型生物活性和药理活性的3-吡唑基噻吩、噻吩并[2,3-d]嘧啶的设计与合成

Design and synthesis of 3-pyrazolyl-thiophene, thieno[2,3-d]pyrimidines as new bioactive and pharmacological activities.

作者信息

Hafez H N, El-Gazzar A B A

机构信息

Photochemistry Department, Heterocyclic and Nucleoside Unit, National Research Centre, Dokki, Giza 12622, Egypt.

出版信息

Bioorg Med Chem Lett. 2008 Oct 1;18(19):5222-7. doi: 10.1016/j.bmcl.2008.08.071. Epub 2008 Aug 26.

Abstract

Two series of 5-ethyl-2-amino-3-pyrazolyl-4-methylthiophenecarboxylate and 2-thioxo-N(3)-aminothieno[2,3-d]pyrimidines were prepared from 3,5-diethyl-2-amino-4-methylthio-phenecaboxylate and evaluated as anti-inflammatory, analgesic and ulcerogenic activities. Among the compounds studied, compounds which containing the substituted hydrazide at C-3 position 7, 16, and 17a showed more potent anti-inflammatory and analgesic activities than the standard drug (Indomethacin and Aspirin), along without ulcerogenity. While compounds 2, 5, 9, 10, and 11c showed moderate activities. Some of the newly synthesized compounds have good to excellent antimicrobial activity.

摘要

由3,5 - 二乙基 - 2 - 氨基 - 4 - 甲硫基 - 苯甲酸酯制备了两系列5 - 乙基 - 2 - 氨基 - 3 - 吡唑基 - 4 - 甲硫基噻吩羧酸酯和2 - 硫代 - N(3) - 氨基噻吩并[2,3 - d]嘧啶,并对其抗炎、镇痛和致溃疡活性进行了评估。在所研究的化合物中,在C - 3位含有取代酰肼的化合物7、16和17a显示出比标准药物(吲哚美辛和阿司匹林)更强的抗炎和镇痛活性,且无致溃疡作用。而化合物2、5、9、10和11c显示出中等活性。一些新合成的化合物具有良好至优异的抗菌活性。

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