通过对新合成的 4-肉桂酰胺基和 2-苯氧基吖啶酰胺基-1H-吡唑-5-基)苯甲酰胺的抗菌、抗生物膜和抗增殖活性进行体外筛选,发现其对白色念珠菌具有很好的抗生物膜活性

IF 2.6 4区 医学 Q3 CHEMISTRY, MEDICINAL
Fabiana Plescia, Valentina Catania, Antonella D’Anneo, Demetrio Raffa, Marianna Lauricella, Domenico Schillaci
{"title":"通过对新合成的 4-肉桂酰胺基和 2-苯氧基吖啶酰胺基-1H-吡唑-5-基)苯甲酰胺的抗菌、抗生物膜和抗增殖活性进行体外筛选,发现其对白色念珠菌具有很好的抗生物膜活性","authors":"Fabiana Plescia,&nbsp;Valentina Catania,&nbsp;Antonella D’Anneo,&nbsp;Demetrio Raffa,&nbsp;Marianna Lauricella,&nbsp;Domenico Schillaci","doi":"10.1007/s00044-024-03224-0","DOIUrl":null,"url":null,"abstract":"<div><p>Several new synthesized 4-cinnamamido- and 2-phenoxyacedamido-(1H-pyrazol-5-yl)benzamides were obtained by two multi step different synthetic routes in order to maximize their yield. The new derivatives were screened to determine the antiproliferative, antimicrobial and antibiofilm activity. The biological results showed how, respect to the antiproliferative and antimicrobial activities, the compounds have a low to missing activity. Different are the results obtained concerning the antibiofilm activity, especially towards <i>Candida albicans</i>. Most of the synthesized compounds showed a good percentage inhibition of biofilm formation ranging from 60 to 73% with a Biofilm Inhibition Concentration 50% (BIC<sub>50</sub>) from 0.13 to 0.01 µM. Among the synthesized compounds the ethyl 5-(4-(2-(4-chlorophenoxy)acetamido)benzamido)-1-methyl-1H-pyrazole-4-carboxylate (<b>27c</b>) resulted the most active molecule with a BIC<sub>50</sub> of 0.01 µM. According to the results obtained, such compound could be considered a lead subject of further studies to obtain novel and more effective antibiofilm agents against <i>C. albicans</i>.</p></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"33 6","pages":"903 - 917"},"PeriodicalIF":2.6000,"publicationDate":"2024-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s00044-024-03224-0.pdf","citationCount":"0","resultStr":"{\"title\":\"A very promising antibiofilm activity against Candida albicans from an in vitro screening for antimicrobial, antibiofilm and antiproliferative activity of new synthesized 4-cinnamamido- and 2-phenoxyacedamido-1H-pyrazol-5-yl)benzamides\",\"authors\":\"Fabiana Plescia,&nbsp;Valentina Catania,&nbsp;Antonella D’Anneo,&nbsp;Demetrio Raffa,&nbsp;Marianna Lauricella,&nbsp;Domenico Schillaci\",\"doi\":\"10.1007/s00044-024-03224-0\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>Several new synthesized 4-cinnamamido- and 2-phenoxyacedamido-(1H-pyrazol-5-yl)benzamides were obtained by two multi step different synthetic routes in order to maximize their yield. The new derivatives were screened to determine the antiproliferative, antimicrobial and antibiofilm activity. The biological results showed how, respect to the antiproliferative and antimicrobial activities, the compounds have a low to missing activity. Different are the results obtained concerning the antibiofilm activity, especially towards <i>Candida albicans</i>. Most of the synthesized compounds showed a good percentage inhibition of biofilm formation ranging from 60 to 73% with a Biofilm Inhibition Concentration 50% (BIC<sub>50</sub>) from 0.13 to 0.01 µM. Among the synthesized compounds the ethyl 5-(4-(2-(4-chlorophenoxy)acetamido)benzamido)-1-methyl-1H-pyrazole-4-carboxylate (<b>27c</b>) resulted the most active molecule with a BIC<sub>50</sub> of 0.01 µM. According to the results obtained, such compound could be considered a lead subject of further studies to obtain novel and more effective antibiofilm agents against <i>C. albicans</i>.</p></div>\",\"PeriodicalId\":699,\"journal\":{\"name\":\"Medicinal Chemistry Research\",\"volume\":\"33 6\",\"pages\":\"903 - 917\"},\"PeriodicalIF\":2.6000,\"publicationDate\":\"2024-05-15\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://link.springer.com/content/pdf/10.1007/s00044-024-03224-0.pdf\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Medicinal Chemistry Research\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://link.springer.com/article/10.1007/s00044-024-03224-0\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Medicinal Chemistry Research","FirstCategoryId":"3","ListUrlMain":"https://link.springer.com/article/10.1007/s00044-024-03224-0","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0

摘要

为了最大限度地提高产率,通过两种多步不同的合成路线获得了几种新合成的 4-肉桂酰胺基和 2-苯氧基酰胺基(1H-吡唑-5-基)苯甲酰胺。对新衍生物进行了筛选,以确定其抗增殖、抗菌和抗生物膜活性。生物学结果表明,在抗增殖和抗菌活性方面,这些化合物的活性较低,甚至没有活性。在抗生物膜活性方面,特别是对白色念珠菌的活性则有所不同。大多数合成化合物对生物膜形成的抑制率在 60% 到 73% 之间,生物膜抑制浓度 50% (BIC50) 为 0.13 到 0.01 µM。在合成的化合物中,5-(4-(2-(4-氯苯氧基)乙酰胺基)苯甲酰胺基)-1-甲基-1H-吡唑-4-羧酸乙酯(27c)是活性最强的分子,其生物抑制浓度 50%为 0.01 µM。根据所获得的结果,这种化合物可被视为进一步研究的先导课题,以获得更有效的新型白僵菌抗生物膜剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

A very promising antibiofilm activity against Candida albicans from an in vitro screening for antimicrobial, antibiofilm and antiproliferative activity of new synthesized 4-cinnamamido- and 2-phenoxyacedamido-1H-pyrazol-5-yl)benzamides

A very promising antibiofilm activity against Candida albicans from an in vitro screening for antimicrobial, antibiofilm and antiproliferative activity of new synthesized 4-cinnamamido- and 2-phenoxyacedamido-1H-pyrazol-5-yl)benzamides

Several new synthesized 4-cinnamamido- and 2-phenoxyacedamido-(1H-pyrazol-5-yl)benzamides were obtained by two multi step different synthetic routes in order to maximize their yield. The new derivatives were screened to determine the antiproliferative, antimicrobial and antibiofilm activity. The biological results showed how, respect to the antiproliferative and antimicrobial activities, the compounds have a low to missing activity. Different are the results obtained concerning the antibiofilm activity, especially towards Candida albicans. Most of the synthesized compounds showed a good percentage inhibition of biofilm formation ranging from 60 to 73% with a Biofilm Inhibition Concentration 50% (BIC50) from 0.13 to 0.01 µM. Among the synthesized compounds the ethyl 5-(4-(2-(4-chlorophenoxy)acetamido)benzamido)-1-methyl-1H-pyrazole-4-carboxylate (27c) resulted the most active molecule with a BIC50 of 0.01 µM. According to the results obtained, such compound could be considered a lead subject of further studies to obtain novel and more effective antibiofilm agents against C. albicans.

求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
Medicinal Chemistry Research
Medicinal Chemistry Research 医学-医药化学
CiteScore
4.70
自引率
3.80%
发文量
162
审稿时长
5.0 months
期刊介绍: Medicinal Chemistry Research (MCRE) publishes papers on a wide range of topics, favoring research with significant, new, and up-to-date information. Although the journal has a demanding peer review process, MCRE still boasts rapid publication, due in part, to the length of the submissions. The journal publishes significant research on various topics, many of which emphasize the structure-activity relationships of molecular biology.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信