Izabella Ventura Souza, Maria Luiza Fróes da Motta Dacome, Andrew Matheus Frederico Rozada, Jonathan Sanches Rosa, Eloisa Gibin Sampiron, Deisiany Gomes Ferreira, Gisele Freitas Gauze, Melyssa Fernanda Norman Negri, Regiane Bertin de Lima Scodro, Rosilene Fressatti Cardoso, Katiany Rizzieri Caleffi-Ferracioli
{"title":"一种具有抗分枝杆菌活性的新型 N-酰腙噁二唑衍生物。","authors":"Izabella Ventura Souza, Maria Luiza Fróes da Motta Dacome, Andrew Matheus Frederico Rozada, Jonathan Sanches Rosa, Eloisa Gibin Sampiron, Deisiany Gomes Ferreira, Gisele Freitas Gauze, Melyssa Fernanda Norman Negri, Regiane Bertin de Lima Scodro, Rosilene Fressatti Cardoso, Katiany Rizzieri Caleffi-Ferracioli","doi":"10.1080/17460913.2024.2412439","DOIUrl":null,"url":null,"abstract":"<p><p><b>Aim:</b> To evaluate the anti<i>-Mycobacterium tuberculosis</i> (<i>Mtb</i>) potential of the hybrid oxadiazol-4-methoxynaphthalene (<b>6n</b>) derived from <i>N</i>-acylhydrazone (<b>4k</b>).<b>Materials & methods:</b> The study determined the minimal inhibitory concentration of (<b>6n)</b> against <i>Mtb</i> H<sub>37</sub>Rv and <i>Mtb</i> clinical isolates, potential combination of (<b>6n)</b> with anti-tuberculosis drugs and carried out time kill curve assay of <i>Mtb</i> H<sub>37</sub>Rv. Additional contribution for the analysis of <b>(6n)</b> was explored by <i>in silico</i> pharmacokinetics, and <i>in vitro</i> and <i>in vivo</i> cytotoxicity determinations.<b>Results:</b> The newly synthesized molecule (<b>6n)</b> demonstrated anti-<i>Mtb</i> activity, low cytotoxicity and selectivity for <i>Mtb.</i><b>Conclusion:</b> The derivative (<b>6n</b>) emerges as a potential anti-TB drug candidate.</p>","PeriodicalId":12773,"journal":{"name":"Future microbiology","volume":null,"pages":null},"PeriodicalIF":2.5000,"publicationDate":"2024-10-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"A new <i>N</i>-acylhydrazone oxadiazole derivative with activity against mycobacteria.\",\"authors\":\"Izabella Ventura Souza, Maria Luiza Fróes da Motta Dacome, Andrew Matheus Frederico Rozada, Jonathan Sanches Rosa, Eloisa Gibin Sampiron, Deisiany Gomes Ferreira, Gisele Freitas Gauze, Melyssa Fernanda Norman Negri, Regiane Bertin de Lima Scodro, Rosilene Fressatti Cardoso, Katiany Rizzieri Caleffi-Ferracioli\",\"doi\":\"10.1080/17460913.2024.2412439\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p><b>Aim:</b> To evaluate the anti<i>-Mycobacterium tuberculosis</i> (<i>Mtb</i>) potential of the hybrid oxadiazol-4-methoxynaphthalene (<b>6n</b>) derived from <i>N</i>-acylhydrazone (<b>4k</b>).<b>Materials & methods:</b> The study determined the minimal inhibitory concentration of (<b>6n)</b> against <i>Mtb</i> H<sub>37</sub>Rv and <i>Mtb</i> clinical isolates, potential combination of (<b>6n)</b> with anti-tuberculosis drugs and carried out time kill curve assay of <i>Mtb</i> H<sub>37</sub>Rv. Additional contribution for the analysis of <b>(6n)</b> was explored by <i>in silico</i> pharmacokinetics, and <i>in vitro</i> and <i>in vivo</i> cytotoxicity determinations.<b>Results:</b> The newly synthesized molecule (<b>6n)</b> demonstrated anti-<i>Mtb</i> activity, low cytotoxicity and selectivity for <i>Mtb.</i><b>Conclusion:</b> The derivative (<b>6n</b>) emerges as a potential anti-TB drug candidate.</p>\",\"PeriodicalId\":12773,\"journal\":{\"name\":\"Future microbiology\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":2.5000,\"publicationDate\":\"2024-10-23\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Future microbiology\",\"FirstCategoryId\":\"99\",\"ListUrlMain\":\"https://doi.org/10.1080/17460913.2024.2412439\",\"RegionNum\":4,\"RegionCategory\":\"生物学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"MICROBIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Future microbiology","FirstCategoryId":"99","ListUrlMain":"https://doi.org/10.1080/17460913.2024.2412439","RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"MICROBIOLOGY","Score":null,"Total":0}
A new N-acylhydrazone oxadiazole derivative with activity against mycobacteria.
Aim: To evaluate the anti-Mycobacterium tuberculosis (Mtb) potential of the hybrid oxadiazol-4-methoxynaphthalene (6n) derived from N-acylhydrazone (4k).Materials & methods: The study determined the minimal inhibitory concentration of (6n) against Mtb H37Rv and Mtb clinical isolates, potential combination of (6n) with anti-tuberculosis drugs and carried out time kill curve assay of Mtb H37Rv. Additional contribution for the analysis of (6n) was explored by in silico pharmacokinetics, and in vitro and in vivo cytotoxicity determinations.Results: The newly synthesized molecule (6n) demonstrated anti-Mtb activity, low cytotoxicity and selectivity for Mtb.Conclusion: The derivative (6n) emerges as a potential anti-TB drug candidate.
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Future Microbiology delivers essential information in concise, at-a-glance article formats. Key advances in the field are reported and analyzed by international experts, providing an authoritative but accessible forum for this increasingly important and vast area of research.
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