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Synthesis, Crystal Structure and Biological Evaluation of 14-O-[(2-chloroacetamide-6-aminopyrimidine-2-yl)thioacetyl] Mutilin

Synthesis, Crystal Structure and Biological Evaluation of 14-O-[(2-chloroacetamide-6-aminopyrimidine-2-yl)thioacetyl] Mutilin
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摘要 The title compound 14-O-[(2-chloroacetamide-6-aminopyrimidine-2-yl) thioacetyl] mutilin(4), C(28)H(39)ClN4O5S, was prepared and characterized by IR, NMR, HRMS and singlecrystal 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)A3, Z = 4, Dc = 1.396 g/cm3, μ(Mo Kα) = 0.462 mm-1, F(000) = 1464, S = 1.003, R = 0.0386 and wR = 0.1014 for 5170 independent reflections(Rint = 0.0224) with I 〉 2σ(I)). The preliminary in vitro antibacterial bioassay against methicillin-resistant Staphylococcus aureus(MRSA-ATCC25923), Staphylococcus 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 μg/m L, respectively. The title compound 14-O-[(2-chloroacetamide-6-aminopyrimidine-2-yl) thioacetyl] mutilin(4), C(28)H(39)ClN4O5S, was prepared and characterized by IR, NMR, HRMS and singlecrystal 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)A3, Z = 4, Dc = 1.396 g/cm3, μ(Mo Kα) = 0.462 mm-1, F(000) = 1464, S = 1.003, R = 0.0386 and wR = 0.1014 for 5170 independent reflections(Rint = 0.0224) with I 〉 2σ(I)). The preliminary in vitro antibacterial bioassay against methicillin-resistant Staphylococcus aureus(MRSA-ATCC25923), Staphylococcus 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 μg/m L, respectively.
出处 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2017年第8期1327-1333,共7页 结构化学(英文)
基金 Supported by Lanzhou Science and Technology Development Project(No.2016-3-101)
关键词 pleuromutilin derivative single-crystal structure antibacterial activities pleuromutilin derivative single-crystal structure antibacterial activities
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