دورية أكاديمية
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Synthesis and evaluation of biological activity for dual-acting antibiotics on the basis of azithromycin and glycopeptides.

التفاصيل البيبلوغرافية
العنوان: Synthesis and evaluation of biological activity for dual-acting antibiotics on the basis of azithromycin and glycopeptides.
المؤلفون: Tevyashova AN; Gause Institute of New Antibiotics, 11 B. Pirogovskaya, Moscow, Russia; D. Mendeleev University of Chemical Technology of Russia, 9 Miusskaya sq., Moscow, Russia. Electronic address: chulis@mail.ru., Bychkova EN; Gause Institute of New Antibiotics, 11 B. Pirogovskaya, Moscow, Russia., Korolev AM; Gause Institute of New Antibiotics, 11 B. Pirogovskaya, Moscow, Russia., Isakova EB; Gause Institute of New Antibiotics, 11 B. Pirogovskaya, Moscow, Russia., Mirchink EP; Gause Institute of New Antibiotics, 11 B. Pirogovskaya, Moscow, Russia., Osterman IA; Department of Chemistry and A.N. Belozersky Institute of Physico-Chemical Biology, M.V. Lomonosov Moscow State University, Leninskie Gory, Moscow, Russia; Centre for Life Sciences, Skolkovo Institute of Science and Technology, Skolkovo, Russia., Erdei R; Department of Organic Chemistry, University of Debrecen, Egyetem ter 1, Debrecen, 4032, Hungary., Szücs Z; Department of Pharmaceutical Chemistry, University of Debrecen, Egyetem ter 1, Debrecen 4032, Hungary., Batta G; Department of Organic Chemistry, University of Debrecen, Egyetem ter 1, Debrecen, 4032, Hungary.
المصدر: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2019 Jan 15; Vol. 29 (2), pp. 276-280. Date of Electronic Publication: 2018 Nov 20.
نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't
اللغة: English
بيانات الدورية: Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE
أسماء مطبوعة: Publication: Oxford : Elsevier Science Ltd
Original Publication: Oxford ; New York : Pergamon Press, c1991-
مواضيع طبية MeSH: Anti-Bacterial Agents/*pharmacology , Azithromycin/*pharmacology , Enterococcus faecalis/*drug effects , Enterococcus faecium/*drug effects , Glycopeptides/*pharmacology , Staphylococcus aureus/*drug effects, Anti-Bacterial Agents/chemical synthesis ; Anti-Bacterial Agents/chemistry ; Azithromycin/chemical synthesis ; Azithromycin/chemistry ; Dose-Response Relationship, Drug ; Glycopeptides/chemical synthesis ; Glycopeptides/chemistry ; Microbial Sensitivity Tests ; Molecular Structure ; Structure-Activity Relationship
مستخلص: One of the promising directions of the combined approach is the design of dual-acting antibiotics - heterodimeric structures on the basis of antimicrobial agents of different classes. In this study a novel series of azithromycin-glycopeptide conjugates were designed and synthesized. The structures of the obtained compounds were confirmed using NMR spectroscopy and mass spectrometry data including MS/MS analysis. All novel hybrid antibiotics were found to be either as active as azithromycin and vancomycin against Gram-positive bacterial strains or have superior activity in comparison with their parent antibiotics. One compound, eremomycin-azithromycin conjugate 16, demonstrated moderate activity against Enterococcus faecium and Enterococcus faecalis strains resistant to vancomycin, and equal to vancomycin's activity for the treatment of mice with Staphylococcus aureus sepsis.
(Copyright © 2018 Elsevier Ltd. All rights reserved.)
فهرسة مساهمة: Keywords: Antibacterial activity; Azithromycin; Dual action antibiotics; Eremomycin; Glycopeptide antibiotics; Macrolide antibiotics; Mechanism of action; Vancomycin
المشرفين على المادة: 0 (Anti-Bacterial Agents)
0 (Glycopeptides)
83905-01-5 (Azithromycin)
تواريخ الأحداث: Date Created: 20181127 Date Completed: 20191104 Latest Revision: 20191104
رمز التحديث: 20221213
DOI: 10.1016/j.bmcl.2018.11.038
PMID: 30473176
قاعدة البيانات: MEDLINE
الوصف
تدمد:1464-3405
DOI:10.1016/j.bmcl.2018.11.038