5,6-顺式青霉烯类：广谱抗耐甲氧西林金黄色葡萄球菌β-内酰胺类抗生素。
5,6-Cis-penems: broad-spectrum anti-methicillin-resistant Staphylococcus aureus beta-lactam antibiotics.
作者信息
Ishiguro M, Tanaka R, Namikawa K, Nasu T, Inoue H, Nakatsuka T, Oyama Y, Imajo S
机构信息
Suntory Institute for Bioorganic Research, Institute for Biomedical Research, Osaka, Japan.
出版信息
J Med Chem. 1997 Jul 4;40(14):2126-32. doi: 10.1021/jm9703348.
5,6-cis-Penem derivatives have been synthesized and evaluated as anti-MRSA antibiotics. The cis-penems 5 and 6 showed potent activities against not only MRSA but also a wide variety of bacteria including beta-lactamase-producing microorganisms. These compounds were designed to have high affinity to the penicillin-binding protein 2a of MRSA and to form stable acyl intermediates with beta-lactamases by blocking the deacylating water molecule.
5,6-顺式青霉烯衍生物已被合成并作为抗耐甲氧西林金黄色葡萄球菌（MRSA）抗生素进行评估。顺式青霉烯5和6不仅对MRSA表现出强效活性，而且对包括产β-内酰胺酶微生物在内的多种细菌也有活性。这些化合物被设计成对MRSA的青霉素结合蛋白2a具有高亲和力，并通过阻断去酰化水分子与β-内酰胺酶形成稳定的酰基中间体。
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