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抗菌和抗真菌剂。十五。联苯苄唑和酮康唑结构类似物的合成及抗真菌活性。

Antibacterial and antifungal agents. XV. Synthesis and antifungal activity of structural analogues of bifonazole and ketoconazole.

作者信息

Stefancich G, Artico M, Ortar G, Silvestri R, Simonetti G, Apuzzo G, Artico M

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Trieste, Italy.

出版信息

Arch Pharm (Weinheim). 1992 Nov;325(11):687-94. doi: 10.1002/ardp.19923251102.

DOI:10.1002/ardp.19923251102
PMID:1485835
Abstract

The synthesis and antifungal activities of the cis- and trans-1-acetyl-4-[4-[[2-(1,1'-biphenyl-4-yl)-2-(1H-imidazol-1-ylmethy l)- 1,3-dioxolan-4-yl]-methoxy]phenyl)piperazines 3 and 4 are reported. Stereochemical assignments to diastereomeric pairs of cis/trans isomers were made on the basis of 1H- and 13C-NMR data. Among test derivatives the best activity was shown by the benzoyl esters of the cis- and trans-[2-(1,1'-biphenyl-4-yl)-2-(1H-imidazol-1-ylmethyl)-1,3-di oxolan-4- yl]methanols 9 and 10.

摘要

报道了顺式和反式-1-乙酰基-4-[4-[[2-(1,1'-联苯-4-基)-2-(1H-咪唑-1-基甲基)-1,3-二氧戊环-4-基]甲氧基]苯基]哌嗪3和4的合成及其抗真菌活性。基于1H-和13C-NMR数据对顺式/反式异构体的非对映体对进行了立体化学归属。在测试的衍生物中,顺式和反式-[2-(1,1'-联苯-4-基)-2-(1H-咪唑-1-基甲基)-1,3-二氧戊环-4-基]甲醇9和10的苯甲酰酯表现出最佳活性。

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