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

摘要

The title compound 14-O-[(2-chloroacetamide-6-aminopyrimidine-2-yl) thioacetyl] mutilin (4),C28H39ClN4OsS,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(MoKα) =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 1 ＞ 2σ(1)).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/mL,respectively.