{"title":"1,4-二氢喹啉席夫碱的新型Β-lactams和噻唑烷酮衍生物:合成、抗菌活性和分子对接研究","authors":"H. Hrichi, Nadia Ali Ahmed Elkanzi, R. Bakr","doi":"10.19261/CJM.2019.647","DOIUrl":null,"url":null,"abstract":"A series of novel isolated β-lactams 3a-c and thiazolidinone derivatives 4a-c were successfully synthesized from reactions of new Schiff's bases 2a-c with chloroacetyl chloride and thioglycolic acid. The chemical structures of the new compounds were confirmed through different spectroscopic techniques including IR, 1 H and 13 C NMR, mass spectrometry and elemental analysis. The antimicrobial activity of the obtained compounds was assessed in vitro against gram-positive Staphylococcus aureus and gram-negative Escherichia coli bacteria and Aspergillus flavus and Candida albicans fungi. All compounds exhibited good to excellent antimicrobial activity against the tested strains. Furthermore, a molecular docking study was carried out for the synthesized compounds and the results indicated that compounds 3b and 4b display comparable binding affinity scores as that of glutamate. These two compounds are promising candidates as antibacterial and antifungal agents that would deserve further investigations.","PeriodicalId":9922,"journal":{"name":"Chemistry Journal of Moldova","volume":"352 1","pages":""},"PeriodicalIF":0.5000,"publicationDate":"2020-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"9","resultStr":"{\"title\":\"Novel Β-lactams and Thiazolidinone Derivatives from 1,4-dihydroquinoxaline Schiff’s Base: Synthesis, Antimicrobial Activity and Molecular Docking Studies\",\"authors\":\"H. Hrichi, Nadia Ali Ahmed Elkanzi, R. Bakr\",\"doi\":\"10.19261/CJM.2019.647\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"A series of novel isolated β-lactams 3a-c and thiazolidinone derivatives 4a-c were successfully synthesized from reactions of new Schiff's bases 2a-c with chloroacetyl chloride and thioglycolic acid. The chemical structures of the new compounds were confirmed through different spectroscopic techniques including IR, 1 H and 13 C NMR, mass spectrometry and elemental analysis. The antimicrobial activity of the obtained compounds was assessed in vitro against gram-positive Staphylococcus aureus and gram-negative Escherichia coli bacteria and Aspergillus flavus and Candida albicans fungi. All compounds exhibited good to excellent antimicrobial activity against the tested strains. Furthermore, a molecular docking study was carried out for the synthesized compounds and the results indicated that compounds 3b and 4b display comparable binding affinity scores as that of glutamate. These two compounds are promising candidates as antibacterial and antifungal agents that would deserve further investigations.\",\"PeriodicalId\":9922,\"journal\":{\"name\":\"Chemistry Journal of Moldova\",\"volume\":\"352 1\",\"pages\":\"\"},\"PeriodicalIF\":0.5000,\"publicationDate\":\"2020-06-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"9\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Chemistry Journal of Moldova\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.19261/CJM.2019.647\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Chemistry Journal of Moldova","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.19261/CJM.2019.647","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
Novel Β-lactams and Thiazolidinone Derivatives from 1,4-dihydroquinoxaline Schiff’s Base: Synthesis, Antimicrobial Activity and Molecular Docking Studies
A series of novel isolated β-lactams 3a-c and thiazolidinone derivatives 4a-c were successfully synthesized from reactions of new Schiff's bases 2a-c with chloroacetyl chloride and thioglycolic acid. The chemical structures of the new compounds were confirmed through different spectroscopic techniques including IR, 1 H and 13 C NMR, mass spectrometry and elemental analysis. The antimicrobial activity of the obtained compounds was assessed in vitro against gram-positive Staphylococcus aureus and gram-negative Escherichia coli bacteria and Aspergillus flavus and Candida albicans fungi. All compounds exhibited good to excellent antimicrobial activity against the tested strains. Furthermore, a molecular docking study was carried out for the synthesized compounds and the results indicated that compounds 3b and 4b display comparable binding affinity scores as that of glutamate. These two compounds are promising candidates as antibacterial and antifungal agents that would deserve further investigations.
期刊介绍:
"Chemistry Journal of Moldova. General, Industrial and Ecological Chemistry" seeks to publish experimental or theoretical research results of outstanding significance and timeliness in all fields of Chemistry, including Industrial and Ecological Chemistry. The main goal of this edition is strengthening the Chemical Society of Moldova, following development of research in Moldovan chemical institutions and promotion of their collaboration with international chemical community. Manuscripts are welcome from all countries.