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带有具有重要生物学意义的吗啉环的新型β-内酰胺的合成及其抗菌和抗疟活性的POM分析

Synthesis of New -Lactams Bearing the Biologically Important Morpholine Ring and POM Analyses of Their Antimicrobial and Antimalarial Activities.

作者信息

Jarrahpour Aliasghar, Heiran Roghayeh, Sinou Véronique, Latour Christine, Djouhri Bouktab Lamia, Michel Brunel Jean, Sheikh Javed, Ben Hadda Taibi

机构信息

Department of Chemistry, College of Sciences, Shiraz University, Shiraz, Iran.

Department of Chemistry, Estahban Higher Education Center, Estahban, Iran.

出版信息

Iran J Pharm Res. 2019 Winter;18(1):34-48.

PMID:31089342
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6487420/
Abstract

Some new lactams bearing biologically important morpholine ring have been synthesized by acylation of amino lactams in the presence of morpholine-4-carbonyl chloride. These novel -lactams were prepared under mild reaction conditions without any solvent in short reaction times. Their biological activities have been examined against microbial agents such as () (), () and fungi such as () and (). They have been also tested against K14 resistant strain and showed moderate to good IC values.

摘要

通过在吗啉 - 4 - 羰基氯存在下对氨基内酰胺进行酰化反应,合成了一些带有具有重要生物学意义的吗啉环的新型内酰胺。这些新型β-内酰胺在温和的反应条件下,无需任何溶剂,在短反应时间内制备而成。已针对诸如()()、()等微生物制剂以及诸如()和()等真菌检测了它们的生物活性。它们还针对K14耐药菌株进行了测试,并显示出中等至良好的IC值。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9aba/6487420/f0b5a1f4ed75/ijpr-18-034-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9aba/6487420/43876908444f/ijpr-18-034-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9aba/6487420/524f1dc80ced/ijpr-18-034-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9aba/6487420/f0b5a1f4ed75/ijpr-18-034-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9aba/6487420/43876908444f/ijpr-18-034-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9aba/6487420/524f1dc80ced/ijpr-18-034-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9aba/6487420/f0b5a1f4ed75/ijpr-18-034-g005.jpg

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Eur J Med Chem. 2011 Oct;46(10):5108-19. doi: 10.1016/j.ejmech.2011.08.025. Epub 2011 Aug 23.
2
Acylating drugs: redesigning natural covalent inhibitors.酰化药物:重新设计天然共价抑制剂。
Curr Opin Chem Biol. 2010 Jun;14(3):421-7. doi: 10.1016/j.cbpa.2010.03.035. Epub 2010 Apr 24.
3
Synthesis of some N-alkyl substituted urea derivatives as antibacterial and antifungal agents.
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J Mol Struct. 2022 Nov 5;1267:133605. doi: 10.1016/j.molstruc.2022.133605. Epub 2022 Jun 28.
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Bioorg Chem. 2022 Mar;120:105587. doi: 10.1016/j.bioorg.2021.105587. Epub 2022 Jan 1.
5
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