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一些 3-(4-(取代)-哌嗪-1-基)肉桂基的合成及生物活性。

Synthesis and biological activity of some 3-(4-(substituted)-piperazin-1-yl)cinnolines.

机构信息

Department of Chemistry, Faculty of Science, University of Jordan, Amman 11942, Jordan.

出版信息

Molecules. 2011 Dec 28;17(1):227-39. doi: 10.3390/molecules17010227.

Abstract

A new series of 6-substituted-4-methyl-3-(4-arylpiperazin-1-yl)cinnolines 8-10 were synthesized as potential antifungal agents via intramolecular cyclization of the respective 1-(2-arylhydrazono)-1-(4-arylpiperazin-1-yl)propan-2-ones 5-7, mediated by polyphosphoric acid (PPA). The amidrazones themselves were synthesized via direct interaction of the appropriate hydrazonoyl chlorides 4a-d with the corresponding N-substituted piperazine in the presence of triethylamine. The structures of the new prepared compounds were confirmed by elemental analyses, (1)H-NMR, (13)C-NMR, and ESI-HRMS spectral data. The antitumor, antibacterial, and antifungal activity of the newly synthesized compounds was evaluated.

摘要

通过多聚磷酸(PPA)介导的各自 1-(2-芳基腙基)-1-(4-芳基哌嗪-1-基)丙烷-2-酮 5-7 的分子内环化,合成了一系列新的 6-取代-4-甲基-3-(4-芳基哌嗪-1-基)肉桂基啶 8-10,作为潜在的抗真菌剂。通过三乙胺存在下合适的腙酰氯 4a-d 与相应的 N-取代哌嗪的直接相互作用,合成了这些腙。新制备的化合物的结构通过元素分析、(1)H-NMR、(13)C-NMR 和 ESI-HRMS 光谱数据得到确认。评估了新合成化合物的抗肿瘤、抗菌和抗真菌活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e584/6268863/97218ba90ba7/molecules-17-00227-g001.jpg

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