{"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, Valentina Catania, Antonella D’Anneo, Demetrio Raffa, Marianna Lauricella, 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, Valentina Catania, Antonella D’Anneo, Demetrio Raffa, Marianna Lauricella, 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}
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.
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.