Eleanor P. Bentley , Oriole W. Song , Ira Glassman , Leepakshi Johar , Cheldon A. Alcantara , Veronica L. Show , Adam R. Johnson , Hendrik Szurmant , David A. Vosburg
{"title":"n -融合咪唑类抗菌剂和细菌拓扑异构酶抑制剂的一锅合成及生物学评价","authors":"Eleanor P. Bentley , Oriole W. Song , Ira Glassman , Leepakshi Johar , Cheldon A. Alcantara , Veronica L. Show , Adam R. Johnson , Hendrik Szurmant , David A. Vosburg","doi":"10.1016/j.rechem.2025.102191","DOIUrl":null,"url":null,"abstract":"<div><div>A series of <em>N</em>-fused imidazoles related to known inhibitors of human topoisomerase IIα were rapidly synthesized by a multicomponent GBB reaction under environmentally friendly conditions with microwave heating. Two of the compounds synthesized exhibited bacteriostatic activity against methicillin-resistant <em>Staphylococcus aureus</em> (MRSA) and other gram-positive bacteria, but none showed significant inhibition of bacterial topoisomerase.</div></div>","PeriodicalId":420,"journal":{"name":"Results in Chemistry","volume":"15 ","pages":"Article 102191"},"PeriodicalIF":4.2000,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"One-pot synthesis and biological evaluation of N-fused imidazoles as antibacterial agents and bacterial topoisomerase inhibitors\",\"authors\":\"Eleanor P. Bentley , Oriole W. Song , Ira Glassman , Leepakshi Johar , Cheldon A. Alcantara , Veronica L. Show , Adam R. Johnson , Hendrik Szurmant , David A. Vosburg\",\"doi\":\"10.1016/j.rechem.2025.102191\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>A series of <em>N</em>-fused imidazoles related to known inhibitors of human topoisomerase IIα were rapidly synthesized by a multicomponent GBB reaction under environmentally friendly conditions with microwave heating. Two of the compounds synthesized exhibited bacteriostatic activity against methicillin-resistant <em>Staphylococcus aureus</em> (MRSA) and other gram-positive bacteria, but none showed significant inhibition of bacterial topoisomerase.</div></div>\",\"PeriodicalId\":420,\"journal\":{\"name\":\"Results in Chemistry\",\"volume\":\"15 \",\"pages\":\"Article 102191\"},\"PeriodicalIF\":4.2000,\"publicationDate\":\"2025-05-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Results in Chemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S2211715625001742\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2025/3/13 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Results in Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S2211715625001742","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/3/13 0:00:00","PubModel":"Epub","JCR":"Q2","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
One-pot synthesis and biological evaluation of N-fused imidazoles as antibacterial agents and bacterial topoisomerase inhibitors
A series of N-fused imidazoles related to known inhibitors of human topoisomerase IIα were rapidly synthesized by a multicomponent GBB reaction under environmentally friendly conditions with microwave heating. Two of the compounds synthesized exhibited bacteriostatic activity against methicillin-resistant Staphylococcus aureus (MRSA) and other gram-positive bacteria, but none showed significant inhibition of bacterial topoisomerase.