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一些含香豆素基团的新型磺酰胺和酰胺衍生物的合成及生物学研究

Synthesis and Biological Investigation of some Novel Sulfonamide and Amide Derivatives Containing Coumarin Moieties.

作者信息

Saeedi Mina, Goli Fereshteh, Mahdavi Mohammad, Dehghan Gholamreza, Faramarzi Mohammad Ali, Foroumadi Alireza, Shafiee Abbas

机构信息

Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medicinal Sciences, Tehran 14176, Iran.

Department of Biology, Faculty of Natural Sciences, University of Tabriz, Iran.

出版信息

Iran J Pharm Res. 2014 Summer;13(3):881-92.

Abstract

New sulfonamide and amide derivatives containing coumarin moieties; oxo-2H-chromen-sulfamoylphenylacetamides and oxo-2H-chromen-arylacetamides were synthesized starting from diverse 2-chloroacetamide derivatives and a wide range of coumarins. The structures of compounds were elucidated by IR and NMR spectra and also analytical elemental analysis. In the next step, the above mentioned compounds were screened for their antimicrobial and antioxidant activities. Their antimicrobial activity was assigned using the conventional agar dilution method and the antioxidant activity was assessed using two methods, 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging method and ferric reducing antioxidant power (FRAP) assay. Although the compounds showed no remarkable antimicrobial activities, most of them exhibited good antioxidant activities. Compounds 5b showed the most potent DPPH activity, whereas 8c was the most efficient compound in FRAP assay.

摘要

含香豆素部分的新型磺胺和酰胺衍生物;氧代-2H-色烯-磺酰基苯基乙酰胺类和氧代-2H-色烯-芳基乙酰胺类化合物是从多种2-氯乙酰胺衍生物和多种香豆素出发合成的。通过红外光谱、核磁共振光谱以及元素分析对化合物的结构进行了阐明。下一步,对上述化合物进行了抗菌和抗氧化活性筛选。采用传统的琼脂稀释法测定其抗菌活性,并用1,1-二苯基-2-苦基肼(DPPH)自由基清除法和铁还原抗氧化能力(FRAP)测定法两种方法评估其抗氧化活性。尽管这些化合物没有表现出显著的抗菌活性,但它们中的大多数都表现出良好的抗氧化活性。化合物5b表现出最强的DPPH活性,而8c是FRAP测定中最有效的化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1d47/4177648/4b1a48f88cf0/ijpr-13-881-g001.jpg

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