具有抗假单胞菌活性的新型广谱头孢菌素。I. 7β-[D-2-[(4-羟基-1,5-萘啶-3-羰基氨基)-和(4-羟基吡啶-3-羰基氨基)]-2-(4-羟基苯基)乙酰胺基]头孢菌素的合成及抗菌活性
New broad-spectrum cephalosporins with anti-pseudomonal activity. I. Synthesis and antibacterial activity of 7 beta-[D-2-[(4-hydroxy-1,5-naphthyridine-3-carbonylamino)- and (4-hydroxypyridine-3-carbonylamino)]-2-(4-hydoxyphenyl)acetamido] cephalosporins.
作者信息
Yamada H, Jimpo K, Tobiki H, Komatsu T, Noguchi H, Irie K, Nakagome T
出版信息
J Antibiot (Tokyo). 1983 May;36(5):522-31. doi: 10.7164/antibiotics.36.522.
The synthesis and the antibacterial activity of 7 beta-[D-2-[(4-hydroxy-1,5-naphthyridine-3-carbonylamino)- and (4-hydroxypyridine-3-carbonylamino)]-2-(4-hydroxyphenyl)acetamido]-cephalosporins with various substituents at the 3-position in the cephem nucleus are described. These compounds exhibited strong antibacterial activities against a variety of Gram-positive and Gram-negative bacteria, including Pseudomonas aeruginosa and Enterobacter aerogenes, which are insensitive to cefazolin and cefmetazole. The compounds (3e, 4e) having a 1-methyl-1H-tetrazolylthiomethyl group at the 3-position appeared to show the best activity in each series. The 4-hydroxypyridine-3-carbonylamino derivative 4e gave higher peak serum concentrations and urinary recovery rates than those of the 4-hydroxy-1,5-naphthyridine derivative 3e when administered subcutaneously to mice and intramuscularly to rats.
描述了在头孢烯核的3-位带有各种取代基的7β-[D-2-[(4-羟基-1,5-萘啶-3-羰基氨基)-和(4-羟基吡啶-3-羰基氨基)]-2-(4-羟基苯基)乙酰胺基]-头孢菌素的合成及其抗菌活性。这些化合物对多种革兰氏阳性和革兰氏阴性细菌表现出强大的抗菌活性，包括对头孢唑林和头孢美唑不敏感的铜绿假单胞菌和产气肠杆菌。在每个系列中，3-位带有1-甲基-1H-四唑基硫甲基的化合物(3e, 4e)似乎表现出最佳活性。当对小鼠皮下给药并对大鼠肌肉注射时，4-羟基吡啶-3-羰基氨基衍生物4e的血清峰值浓度和尿回收率高于4-羟基-1,5-萘啶衍生物3e。
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