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Convenient Synthesis and Antimicrobial Activity of New 3-Substituted 5-(Benzofuran-2-yl)-pyrazole Derivatives
Archiv der Pharmazie ( IF 5.1 ) Pub Date : 2008-11-01 , DOI: 10.1002/ardp.200800119
Bakr F Abdel-Wahab 1 , Hatem A Abdel-Aziz , Essam M Ahmed
Affiliation  

The reaction of ethyl 4‐(benzofuran‐2‐yl)‐2,4‐dioxobutanoate 2 with two moles of hydrazine hydrate afforded 5‐(benzofuran‐2‐yl)‐1H‐pyrazole‐3‐carbohydrazide 4a, while its reaction with equimolar amount of phenylhydrazine gave ester 3b which then converted to 5‐(benzofuran‐2‐yl)‐1‐phenyl‐1H‐pyrazole‐3‐carbohydrazide 4b. Various new compounds such as imides 5 and 6, acyl hydrazones 7 and 8, bi‐pyrazoles 9‐12, and 1,3‐thiazole derivatives 14 and 15 were prepared from carbohydrazide derivatives 4a, b. The new compounds are tested for their antimicrobial activity. Compounds 2, 5, 7, and 8 showed antifungal activities against C. albicans. Also, compounds 2, 6, 8, and 15 showed antibacterial activities.

中文翻译:

新型 3-取代 5-(苯并呋喃-2-基)-吡唑衍生物的简便合成及抗菌活性

4-(苯并呋喃-2-基)-2,4-二氧代丁酸乙酯2与2摩尔水合肼反应得到5-(苯并呋喃-2-基)-1H-吡唑-3-碳酰肼4a,而其与等摩尔量的苯肼生成酯 3b,然后将其转化为 5-(苯并呋喃-2-基)-1-苯基-1H-吡唑-3-碳酰肼 4b。由碳酰肼衍生物 4a、b 制备了各种新化合物,如酰亚胺 5 和 6、酰基腙7 和 8、双吡唑 9-12 和 1,3-噻唑衍生物 14 和 15。测试新化合物的抗微生物活性。化合物 2、5、7 和 8 显示出对白色念珠菌的抗真菌活性。此外,化合物 2、6、8 和 15 显示出抗菌活性。
更新日期:2008-11-01
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