抗耐甲氧西林金黄色葡萄球菌头孢菌素。第1部分：C-3取代的硫代吡啶鎓衍生物。
Anti-MRSA cephems. Part 1: C-3 substituted thiopyridinium derivatives.
作者信息
Springer D M, Luh B Y, Bronson J J
机构信息
Anti-infective Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492, USA.
出版信息
Bioorg Med Chem Lett. 2001 Mar 26;11(6):797-801. doi: 10.1016/s0960-894x(01)00060-9.
Sixteen novel cephalosporin derivatives with activity against methicillin-resistant Staphylococcus aureus (MRSA) are described. The compounds were synthesized using substituted thiopyridones, generated either by cyclization of functionalized precursors, or by direct alkylation of the enolate of 2-methyl substituted pyrones. The most active compound in vitro against a strain of MRSA (A27223) displayed an MIC of 0.5 microg/mL. The most efficacious compound in vivo had a PD50 of 2.1 mg/kg.
描述了16种对耐甲氧西林金黄色葡萄球菌（MRSA）具有活性的新型头孢菌素衍生物。这些化合物是使用取代的硫代吡啶酮合成的，取代的硫代吡啶酮要么通过官能化前体的环化产生，要么通过2-甲基取代的吡喃酮烯醇盐的直接烷基化产生。体外对一株MRSA（A27223）活性最高的化合物的最低抑菌浓度（MIC）为0.5微克/毫升。体内最有效的化合物的半数有效剂量（PD50）为2.1毫克/千克。
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