Synthesis, Crystal Structure And Biological E.valuation Of 14-O-[(2-Chloroacetamide-6-Aminopyrimidine-2-Yl)Thioacetyl] Mutilin
文献类型: 外文期刊
作者: Wang Liang;Zhou Xiang;Shang Ruo-Feng;Yi Yun-Peng;Wang Liang;Xin Zhi-Jun;Liang Jian-Ping;Lu Xi-Hong;Li Xue-Hu
作者机构:
关键词: pleuromutilin derivative; single-crystal structure; antibacterial activities
期刊名称: CHINESE JOURNAL OF STRUCTURAL CHEMISTRY
ISSN: 0254-5861
年卷期: 2017 年 36 卷 8 期
页码:
摘要: The title compound 14-O-[(2-chloroacetamide-6-aminopyrimidine-2-yl) thioacetyl] mutilin (4), C28H39ClN4O5S, was prepared and characterized by IR, NMR, HRMS and single- crystal X-ray diffraction. The title compound crystallizes in orthorhombic system, space group P212121 with a = 11.5388(8), b = 14.5282(10), c = 19.8301(14) A, V = 3324.3(4) A(3), Z = 4, D-c = 1.396 g/cm(3), mu(MoK alpha) = 0.462 mm(-1), F(000) = 1464, S = 1.003, R = 0.0386 and wR = 0.1014 for 5170 independent reflections (R-int = 0.0224) with I > 2 sigma(I)). The preliminary in vitro antibacterial bioassay against methicillin-resistant Staphylococcus aureus (MRSA-ATCC25923), Staphylo- coccus aureus (S. aureus), Escherichia coli (E. coli), and Staphylococcus warneri (S .warneri) were screened and the MIC values of the title compound were 0.125, 0.0625, 8 and 0.5 mu g/mL, respectively.
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