دورية أكاديمية
Novel effective antibacterial small-molecules against Staphylococcus and Enterococcus strains.
العنوان: | Novel effective antibacterial small-molecules against Staphylococcus and Enterococcus strains. |
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المؤلفون: | Yasrebi K; Institute of Pharmacy, Martin Luther University Halle-Wittenberg, 06120 Halle, Germany., Schade N; Institute of Pharmacy, Martin Luther University Halle-Wittenberg, 06120 Halle, Germany., Adeniyi ET; Institute of Molecular Infection Biology, Julius Maximilians University Wuerzburg, 97080 Wuerzburg, Germany., Wecklein B; Institute of Molecular Infection Biology, Julius Maximilians University Wuerzburg, 97080 Wuerzburg, Germany., Ymeraj A; Institute of Molecular Infection Biology, Julius Maximilians University Wuerzburg, 97080 Wuerzburg, Germany., Hertlein T; Institute of Molecular Infection Biology, Julius Maximilians University Wuerzburg, 97080 Wuerzburg, Germany., Ohlsen K; Institute of Molecular Infection Biology, Julius Maximilians University Wuerzburg, 97080 Wuerzburg, Germany., Suzen S; Faculty of Pharmacy, Ankara University, 06100 Ankara, Turkey., Lalk M; Institute of Biochemistry, Ernst Moritz Arndt University Greifswald, 17487 Greifswald, Germany., Ströhl D; Institute of Chemistry, Martin Luther University Halle-Wittenberg, 06120 Halle, Germany., Hilgeroth A; Institute of Pharmacy, Martin Luther University Halle-Wittenberg, 06120 Halle, Germany. |
المصدر: | Future medicinal chemistry [Future Med Chem] 2020 Jul; Vol. 12 (13), pp. 1205-1211. Date of Electronic Publication: 2020 Jun 09. |
نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
اللغة: | English |
بيانات الدورية: | Publisher: Future Science Country of Publication: England NLM ID: 101511162 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1756-8927 (Electronic) Linking ISSN: 17568919 NLM ISO Abbreviation: Future Med Chem Subsets: MEDLINE |
أسماء مطبوعة: | Original Publication: London : Future Science, 2009- |
مواضيع طبية MeSH: | Anti-Bacterial Agents/*pharmacology , Enterococcus/*drug effects , Hydrocarbons, Brominated/*pharmacology , Hydrocarbons, Iodinated/*pharmacology , Small Molecule Libraries/*pharmacology , Staphylococcus/*drug effects, Anti-Bacterial Agents/chemical synthesis ; Anti-Bacterial Agents/chemistry ; Hydrocarbons, Brominated/chemical synthesis ; Hydrocarbons, Brominated/chemistry ; Hydrocarbons, Iodinated/chemical synthesis ; Hydrocarbons, Iodinated/chemistry ; Microbial Sensitivity Tests ; Molecular Structure ; Small Molecule Libraries/chemical synthesis ; Small Molecule Libraries/chemistry |
مستخلص: | Background: Resistance developments against established antibiotics are an emerging problem for antibacterial therapies. Novel antibiotics are urgently needed. Materials & methods: We developed novel small-molecule antibacterials which are easily accessible in a simple one-pot synthesis. The central cyclopentaindole core is substituted with two indole residues. Various indole and cyclopentane substituents have been introduced. Additionally, first indole substituted propene compounds as ring-open variants of the cyclopentaindoles have been yielded and evaluated as antibacterials against Staphylococcus aureus and Enterococcus strains. Results: Most effective compounds have been those with a bromo cyclopentane and a chloro indole substitution. First lead compounds were identified with promising activities similar to that observed in vitro for last resort antibiotics, so that the novel compounds enriche the pool of perspective small-molecule antibacterial drug candidates. |
فهرسة مساهمة: | Keywords: Enterococcus; Staphylococcus; antibacterial activity; compound evaluation; lead structure; structure-dependent activity |
المشرفين على المادة: | 0 (Anti-Bacterial Agents) 0 (Hydrocarbons, Brominated) 0 (Hydrocarbons, Iodinated) 0 (Small Molecule Libraries) |
تواريخ الأحداث: | Date Created: 20200610 Date Completed: 20210713 Latest Revision: 20210713 |
رمز التحديث: | 20221213 |
DOI: | 10.4155/fmc-2020-0010 |
PMID: | 32515228 |
قاعدة البيانات: | MEDLINE |
تدمد: | 1756-8927 |
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DOI: | 10.4155/fmc-2020-0010 |