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Recent advances in the synthesis and applications of furocoumarin derivatives

中国化学快报:英文版 2023年第9期34卷 119-133页

作者： Chaoyue Chen Zheng-Bin Tang Zhichang Liu School of Chemistry and Chemical Engineering Jiangsu University of TechnologyChangzhou 213001China Key Laboratory of Precise Synthesis of Functional Molecules of Zhejiang Province Department of ChemistrySchool of Science and Research Center for Industries of the FutureWestlake Universityand Westlake Institute for Advanced StudyHangzhou 310030China

Furocoumarins are an important class of heterocyclic compounds with a fused tricyclic structure of coumarin and furan *** are commonly found in bioactive natural products and have a diverse range of biological and pharmaceutical properties,including cytotoxicity,photosensitivity,insecticidal,antibacterial,and antifungal activity,among *** elegant linear/angular tricyclic skeleton and superior pharmacological properties,make them ideal for building and developing advanced biological scaffolds for biomedical *** a result,the family of furocoumarins has been the focus of intensive research,and lots of encouraging progress have been achieved in recent *** review summarizes the most recent methods reported for the synthesis of the furocoumarin derivative family,along with their applications in medicinal chemistry covering from 2018 to 2022.

关键词： Furocoumarin Coumarin Furan Synthesis pharmaceutical activity Applications

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Evaluation of pharmaceutical activities of G-protein coupled receptor targeted pharmaceuticals in Chinese wastewater effluent

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Chinese Chemical Letters 2020年第10期31卷 2859-2863页

作者： Han Zhang Yingchao Lin Zhengyu Men Masaru Ihara Weizun Li Kai He College of Environmental Science and Engineering Nankai UniversityTianjin 300071China Research Center for Environmental Quality Management Kyoto UniversityOtsu 5200811Japan

The occurre nce of biologically active pharmaceuticals in aquatic enviro nments raised the potential risks to aquatic *** these marketed biological active pharmaceuticals,it has been estimated that40%of them target G-protein-coupled receptors(GPCRs).We have illustrated pharmaceutical activities of GPCR targeted pharmaceuticals in English and Japanese wastewater by the in vitro transforming growth factor-α(TGFα)shedding ***,as the most important producer and consumer of pharmaceuticals,the occurrence of GPCR targeted pharmaceuticals in China had remained *** this study,we investigated the pharmaceutical activities of GPCR targeted pharmaceuticals in secondary effluents of Chinese wastewater treatment *** discovered antagonistic activities against angiotensin(AT1)receptor at up to 7.2×102 ng-valsartan-equivalent quantity/L in Chinese wastewater for the first time as well as agonistic activities against dopamine(D2)***,in parallel with the assay,we determined concentrations of GPCR targeted pharmaceuticals in target wastewater by liquid chromatography coupled with tandem mass spectrometry(LC-MS/MS).Through the comparison of predicted antagonistic activities calculated by concentrations and potency values from the assay,we found that the measured antagonistic activities against AT1 receptor from the assay were higher than the predicted AT1 activities from valsartan,irbesartan,and losartan,indicating the potential existence of other unknown AT1 antagonists in wastewater.

关键词： PCR targeted pharmaceutical pharmaceutical activity TGFαshedding assay Wastewater

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