Jorgensen J H, Redding J S, Maher L A
Department of Pathology, University of Texas Health Science Center, San Antonio 78284.
Antimicrob Agents Chemother. 1988 Oct;32(10):1477-80. doi: 10.1128/AAC.32.10.1477.
A new carbacephem analog of cefaclor, LY163892, was examined along with four other cephalosporins for chemical stability and for antibacterial activity under a variety of susceptibility test conditions. LY163892 was found to be markedly more stable than cefaclor during storage at 4 and 35 degrees C in human serum, human urine, and various bacteriological media. Under these conditions, LY163892 demonstrated stability equal or superior to the stabilities of cephalexin, cephalothin, and cefuroxime. Broth and agar dilution susceptibility tests did not reveal significant differences in LY163892 activity in a variety of test media, although LY163892 MICs were somewhat higher in Mueller-Hinton chocolate agar or Trypticase soy broth (BBL Microbiology Systems, Cockeysville, Md.) than in other media. The activity of LY163892 against selected pathogens was only slightly influenced by the increased or decreased pH of the test medium, in a manner similar to that of the other cephalosporins tested. Thus, the carbacephem structure of LY163892 appears to represent a more stable cephalosporin than cefaclor, while retaining a similar antimicrobial spectrum.
将头孢克洛的一种新型碳头孢烯类似物LY163892与其他四种头孢菌素一起,在各种药敏试验条件下检测其化学稳定性和抗菌活性。结果发现,在4℃和35℃下于人体血清、人体尿液及各种细菌学培养基中储存时,LY163892比头孢克洛明显更稳定。在这些条件下,LY163892表现出的稳定性等同于或优于头孢氨苄、头孢噻吩和头孢呋辛。肉汤稀释法和琼脂稀释法药敏试验未显示LY163892在各种试验培养基中的活性有显著差异,不过LY163892在穆勒-欣顿巧克力琼脂或胰蛋白酶大豆肉汤(BBL微生物系统公司,马里兰州科基斯维尔)中的最低抑菌浓度(MIC)比在其他培养基中略高。LY163892对选定病原体的活性仅受试验培养基pH值升高或降低的轻微影响,其方式与所检测的其他头孢菌素类似。因此,LY163892的碳头孢烯结构似乎代表一种比头孢克洛更稳定的头孢菌素,同时保留了相似的抗菌谱。