دورية أكاديمية
Design, synthesis and antibacterial activities of pleuromutilin derivatives.
| العنوان: | Design, synthesis and antibacterial activities of pleuromutilin derivatives. |
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| المؤلفون: | Liu HX; College of Pharmacy, Hebei University of Chinese Medicine, Shijiazhuang 050200, China., Ma DL; College of Pharmacy, Hebei University of Chinese Medicine, Shijiazhuang 050200, China., Cui G; College of Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology, Shijiazhuang 050018, China., Zhang Y; College of Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology, Shijiazhuang 050018, China., Xue FQ; Shanghai Veterinary Research Institute, Chinese Academy of Agricultural Sciences, Shanghai 200241, China. |
| المصدر: | Journal of Asian natural products research [J Asian Nat Prod Res] 2021 Feb; Vol. 23 (2), pp. 123-137. Date of Electronic Publication: 2020 Feb 06. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Informa Healthcare Country of Publication: England NLM ID: 100888334 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1477-2213 (Electronic) Linking ISSN: 10286020 NLM ISO Abbreviation: J Asian Nat Prod Res Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: London : Informa Healthcare Original Publication: [Newark, N.J.?] : Harwood Academic Publishers, |
| مواضيع طبية MeSH: | Anti-Infective Agents* , Staphylococcus aureus*, Anti-Bacterial Agents/pharmacology ; Diterpenes ; Microbial Sensitivity Tests ; Molecular Structure ; Polycyclic Compounds ; Structure-Activity Relationship ; Pleuromutilins |
| مستخلص: | We described the design, synthesis and antimicrobial activities of novel pleuromutilin derivatives with substituted piperazine substrate. Minimum inhibitory concentration (MIC) was used to evaluate the activity of the derivatives against six bacteria in vitro , and compound 8 was potent against Staphylococcus aureus and Staphylococcus epidermidis with the MIC value of 0.0625 μg/ml. 10a and 10 b showed similar activity to positive control drugs (tiamulin, erythromycin) against S. aureus with the MIC value of 0.125 μg/ml. The binding mode of compound 8 and tiamulin to the ribosome pocket showed the correlation between binding parameters and the antibacterial activity, and more bonds and stronger combination could effectively enhance the activity of compounds.[Formula: see text]. |
| فهرسة مساهمة: | Keywords: Gram-positive bacteria; Pleuromutilin derivatives; antibacterial activity; design; synthesis |
| المشرفين على المادة: | 0 (Anti-Bacterial Agents) 0 (Anti-Infective Agents) 0 (Diterpenes) 0 (Polycyclic Compounds) |
| تواريخ الأحداث: | Date Created: 20200207 Date Completed: 20210506 Latest Revision: 20231213 |
| رمز التحديث: | 20231215 |
| DOI: | 10.1080/10286020.2020.1713764 |
| PMID: | 32024387 |
| قاعدة البيانات: | MEDLINE |
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Full Text Finder | تدمد: | 1477-2213 |
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| DOI: | 10.1080/10286020.2020.1713764 |