Neu H C, Saha G, Chin N X
Department of Medicine, College of Physicians and Surgeons, Columbia University, New York, New York 10032.
Antimicrob Agents Chemother. 1989 Oct;33(10):1795-800. doi: 10.1128/AAC.33.10.1795.
FK482 is an oral aminothiazolyl hydroxyimino cephalosporin with a C-3 vinyl group. Its activity was compared with those of cephalexin, cefuroxime, cefixime, and amoxicillin-clavulanate. FK482 inhibited 90% of Staphylococcus aureus isolates at 1 micrograms/ml and 90% of Streptococcus pyogenes, Streptococcus agalactiae, and Streptococcus pneumoniae isolates at less than or equal to 0.012 micrograms/ml, superior to cephalexin and cefuroxime and similar to cefixime. It did not inhibit oxacillin-resistant S. aureus. FK482 inhibited 90% of Enterococcus faecalis isolates at 8 micrograms/ml. Although 90% of Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Salmonella species, and Shigella species isolates were inhibited by less than or equal to 2 micrograms/ml, FK482 was less active than cefixime against Citrobacter, Enterobacter, Morganella, Serratia, and Providencia species, with MICs for many isolates of greater than 8 micrograms/ml. FK482 inhibited Haemophilus influenzae and Neisseria gonorrhoeae at concentrations comparable to that of cefixime and superior to those of cephalexin and cfaclor. Bacteroides and Pseudomonas species were resistant. FK482 was not hydrolyzed by the TEM-1 and TEM-2 beta-lactamases but was hydrolyzed by TEM-3 and the Proteus vulgaris enzyme. It had a high affinity for chromosomal beta-lactamases.
FK482是一种带有C-3乙烯基的口服氨噻唑基羟亚氨基头孢菌素。将其活性与头孢氨苄、头孢呋辛、头孢克肟和阿莫西林-克拉维酸进行了比较。FK482对1微克/毫升的金黄色葡萄球菌分离株的抑菌率达90%，对化脓性链球菌、无乳链球菌和肺炎链球菌分离株的抑菌率在小于或等于0.012微克/毫升时达90%，优于头孢氨苄和头孢呋辛，与头孢克肟相似。它对耐苯唑西林的金黄色葡萄球菌没有抑制作用。FK482对8微克/毫升的粪肠球菌分离株的抑菌率达90%。虽然90%的大肠埃希菌、肺炎克雷伯菌、奇异变形杆菌、沙门菌属和志贺菌属分离株在小于或等于2微克/毫升时被抑制，但FK482对柠檬酸杆菌属、肠杆菌属、摩根菌属、沙雷菌属和普罗威登斯菌属的活性低于头孢克肟，许多分离株的最低抑菌浓度大于8微克/毫升。FK482对流感嗜血杆菌和淋病奈瑟菌的抑制浓度与头孢克肟相当，优于头孢氨苄和头孢克洛。拟杆菌属和假单胞菌属具有耐药性。FK482不被TEM-1和TEM-2β-内酰胺酶水解，但被TEM-3和普通变形杆菌的酶水解。它对染色体β-内酰胺酶具有高亲和力。
