Omura S, Matsubara H, Tsuzuki K, Nakagawa A
J Antibiot (Tokyo). 1984 Sep;37(9):1007-15. doi: 10.7164/antibiotics.37.1007.
Thioether derivatives of tylosin and demycarosyltylosin were synthesized by Michael-type addition of thiol to C-11 of the enone moiety on the aglycone. Some of tylosin derivatives were effective to macrolide resistant Staphylococcus aureus, and their in vivo activities were same or superior than that of tylosin.
通过硫醇对糖苷配基上烯酮部分的C-11进行迈克尔型加成反应,合成了泰乐菌素和去碳霉糖泰乐菌素的硫醚衍生物。一些泰乐菌素衍生物对耐大环内酯类金黄色葡萄球菌有效,其体内活性与泰乐菌素相同或优于泰乐菌素。