{"title":"氟化2-羟基萘-1-羧基苯胺的光合抑制活性","authors":"T. Goněc, M. Oravec, J. Jampílek","doi":"10.3390/ecsoc-25-11652","DOIUrl":null,"url":null,"abstract":": 2-Hydroxy- N -phenylnaphthalene-1-carboxamide, three fluoro monosubstituted and five fluoro disubstituted 2-hydroxynaphthalene-1-carboxanilides were prepared by microwave-assisted synthesis and characterized. All the compounds were evaluated for their ability to inhibit photosynthetic electron transport (PET) in spinach ( Spinacia oleracea L.) chloroplasts. The PET inhibitory activity of the discussed compounds proved to be in a wide range, from inactive N -(2,6-difluorophenyl)-2-hydroxynaphthalene-1-carboxamide with an IC 50 = 904 µ M to N -(2,5-difluorophenyl)-2-hydroxynaphthalene-1-carboxamide with an IC 50 of 44.2 µ M, which was the most potent isomer of the series of evaluated compounds. Based on previous studies, it can be assumed that the mechanism of PET inhibition of these compounds is the inhibition of photosystem II in the thylakoid membrane.","PeriodicalId":11441,"journal":{"name":"ECSOC-25","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2021-11-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Photosynthesis-Inhibiting Activity of Fluorinated 2-Hydroxynaphthalene-1-carboxanilides\",\"authors\":\"T. Goněc, M. Oravec, J. Jampílek\",\"doi\":\"10.3390/ecsoc-25-11652\",\"DOIUrl\":null,\"url\":null,\"abstract\":\": 2-Hydroxy- N -phenylnaphthalene-1-carboxamide, three fluoro monosubstituted and five fluoro disubstituted 2-hydroxynaphthalene-1-carboxanilides were prepared by microwave-assisted synthesis and characterized. All the compounds were evaluated for their ability to inhibit photosynthetic electron transport (PET) in spinach ( Spinacia oleracea L.) chloroplasts. The PET inhibitory activity of the discussed compounds proved to be in a wide range, from inactive N -(2,6-difluorophenyl)-2-hydroxynaphthalene-1-carboxamide with an IC 50 = 904 µ M to N -(2,5-difluorophenyl)-2-hydroxynaphthalene-1-carboxamide with an IC 50 of 44.2 µ M, which was the most potent isomer of the series of evaluated compounds. Based on previous studies, it can be assumed that the mechanism of PET inhibition of these compounds is the inhibition of photosystem II in the thylakoid membrane.\",\"PeriodicalId\":11441,\"journal\":{\"name\":\"ECSOC-25\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2021-11-13\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"ECSOC-25\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.3390/ecsoc-25-11652\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"ECSOC-25","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.3390/ecsoc-25-11652","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0
摘要
采用微波辅助合成方法制备了2-羟基- N -苯基萘-1-羧酰胺、3个氟单取代和5个氟二取代的2-羟基萘-1-羧苯胺并对其进行了表征。所有化合物对菠菜叶绿体光合电子传递(PET)的抑制能力进行了评价。所讨论的化合物的PET抑制活性范围很广,从无活性的N -(2,6-二氟苯基)-2-羟基萘-1-羧酰胺(IC 50 = 904µM)到N -(2,5-二氟苯基)-2-羟基萘-1-羧酰胺(IC 50为44.2µM),是该系列化合物中最有效的异构体。根据以往的研究,可以认为PET抑制这些化合物的机制是抑制类囊体膜中的光系统II。
Photosynthesis-Inhibiting Activity of Fluorinated 2-Hydroxynaphthalene-1-carboxanilides
: 2-Hydroxy- N -phenylnaphthalene-1-carboxamide, three fluoro monosubstituted and five fluoro disubstituted 2-hydroxynaphthalene-1-carboxanilides were prepared by microwave-assisted synthesis and characterized. All the compounds were evaluated for their ability to inhibit photosynthetic electron transport (PET) in spinach ( Spinacia oleracea L.) chloroplasts. The PET inhibitory activity of the discussed compounds proved to be in a wide range, from inactive N -(2,6-difluorophenyl)-2-hydroxynaphthalene-1-carboxamide with an IC 50 = 904 µ M to N -(2,5-difluorophenyl)-2-hydroxynaphthalene-1-carboxamide with an IC 50 of 44.2 µ M, which was the most potent isomer of the series of evaluated compounds. Based on previous studies, it can be assumed that the mechanism of PET inhibition of these compounds is the inhibition of photosystem II in the thylakoid membrane.