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（E）-和（Z）-咪唑基苯并二氢吡喃酮肟醚的立体选择性合成及体外抗真菌活性评价

Stereoselective synthesis and in vitro antifungal evaluation of (E)- and (Z)-imidazolylchromanone oxime ethers.

作者信息

Emami Saeed, Falahati Mehraban, Banifatemi Ali, Moshiri Kayvan, Shafiee Abbas

机构信息

Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Iran.

出版信息

Arch Pharm (Weinheim). 2002 Jul;335(7):318-24. doi: 10.1002/1521-4184(200209)335:7<318::AID-ARDP318>3.0.CO;2-O.

DOI:10.1002/1521-4184(200209)335:7<318::AID-ARDP318>3.0.CO;2-O
PMID:12207281
Abstract

A series of (E)- and (Z)-2, 3-dihydro-3-(1H-imidazol-1-yl)-4H-1-benzopyran-4-one oxime ethers have been synthesized and tested for antifungal activity. Most compounds showed moderate to potent in vitro antifungal activity. Among the tested compounds, compound (E)-3d was the most active agent against Candida albicans and Aspergillus niger, and compounds (Z)-(3a) and (E)-3a were the most potent compounds against Microsporum gypseum. Detailed stereoselective synthesis, spectroscopic, and biological data are reported.

摘要

合成了一系列（E）-和（Z）-2,3-二氢-3-（1H-咪唑-1-基）-4H-1-苯并吡喃-4-酮肟醚，并测试了其抗真菌活性。大多数化合物表现出中度至强效的体外抗真菌活性。在测试的化合物中，化合物（E）-3d是对白色念珠菌和黑曲霉最具活性的药剂，化合物（Z）-（3a）和（E）-3a是对石膏样小孢子菌最有效的化合物。报道了详细的立体选择性合成、光谱和生物学数据。

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