抗耐甲氧西林金黄色葡萄球菌头孢菌素。第2部分：C-7肉桂酸衍生物。
Anti-MRSA cephems. Part 2: C-7 cinnamic acid derivatives.
作者信息
Springer Dane M, Luh Bing Yu, Goodrich Jason, Bronson Joanne J
机构信息
Anti-infective Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, PO Box 5100, Wallingford, CT 06492, USA.
出版信息
Bioorg Med Chem. 2003 Jan 17;11(2):265-79. doi: 10.1016/s0968-0896(02)00336-x.
Forty-five novel cephalosporin derivatives with activity against methicillin-resistant Staphylococcus aureus (MRSA) are described. The compounds contain novel cinnamic acid moieties at C-7 that were synthesized using a key Heck reaction followed by nucleophilic aromatic substitution reactions. The most active compound (41) displayed an MIC(90) against MRSA of 1.0 microg/mL, and a PD(50) of 0.8 mg/kg. Compound 14 was found to be very safe in a mouse model of acute toxicity.
本文描述了45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。这些化合物在C-7位含有新型肉桂酸部分，通过关键的Heck反应，随后进行亲核芳香取代反应合成。活性最高的化合物（41）对MRSA的MIC(90)为1.0μg/mL，PD(50)为0.8mg/kg。在急性毒性小鼠模型中发现化合物14非常安全。
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