Synthesis and antimicrobial evaluation of 1-(benzofuran-2-yl)-4-nitro-3-arylbutan-1-ones and 3-(benzofuran-2-yl)-4,5-dihydro-5-aryl-1-[4-(aryl)-1, 3-thiazol-2-yl]-1H-pyrazoles

被引：219

作者：

Abdel-Wahab, Bakr F. ^{[1
]}

Abdel-Aziz, Hatem A. ^{[1
]}

Ahmed, Essam M. ^{[2
]}

机构：

[1] Natl Res Ctr, Appl Organ Chem Dept, Giza, Egypt

[2] Natl Res Ctr, Nat & Microbial Prod Chem Dept, Giza, Egypt

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 06期

关键词：

Benzofuran; Nitromethane; Thiazolyl-pyrazoline; Antimicrobial activity; THIAZOLYL-PYRAZOLINE DERIVATIVES; ANTIBACTERIAL ACTIVITY; BENZOFURAN; AGENTS; ANTIFUNGAL;

D O I：

10.1016/j.ejmech.2008.09.029

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2-Acetylbenzofuran 1 on treatment with substituted aldehydes affords the corresponding chalcones 2a-c. Treatment of the chalcones with nitromethane under Michael addition condition furnished the corresponding Michael adducts 3a-c. Cyclocondensation of the chalcones 2a and 2b with thiosemicarbazide under basic refluxing conditions gave 3-(benzofuran-2-yl)-5-(4-aryl)-4,5-dihydropyrazole-1-carbothioamides 4a,b. The pyrazolines 7a-d were synthesized by treating 4a,b with phenacyl bromides in refluxing ethanol. All the synthesized compounds were screened for their antibacterial and antifungal activities at 100 mu g concentration. Some of our compounds showed excellent antimicrobial activities than control drugs. (C) 2008 Elsevier Masson SAS. All rights reserved.

引用

页码：2632 / 2635

页数：4

共 36 条

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