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KMID : 0903519970400020157
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Journal of the Korean Society of Agricultural Chemistry and Biotechnology
1997 Volume.40 No. 2 p.157 ~ p.162
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In vivo Evaluation of a Novel B-Lactam Antibiotics , YH-487
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이종욱/Lee, Jong Wook
정동효/원유정/강희일/Chung, Dong Hyo/Won, Yu Jung/Kang, Heui Il
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Abstract
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A novel compound, named YH-487, was synthesized by attaching the thiol and aminothiazole residue to C₃ and C_7 position of 7-aminocephalosporanic acid (7-ACA). The therapeutic efficacy on infected animals, pharmacokinetics in vivo and the effect on intestinal microflora of YH-487 were examined. The pharmacokinetics of YH-487 were similar to that of cefotaxime, a third generation β-lactam antibiotics, in rat. Upon in vivo administration, YH-487 was predominantly delivered to kidney, and mostly excreted through kidney without making any metabolites. The therapeutic efficacy of YH-487 to animal infected with E. coli was three times and twenty times higher than that of cefotaxime and cefotiam, respectively. In vivo administration of YH-487 to Sprague-Dawley rats significantly decreased the population of intestinal gram negative species such as Enterobacteria and Bacteroides. However, no significant changes were observed in gram positive species such as Lactobacillus, Bifidobacteria and Staphylococcus. In addition, continuous administration of YH-487 did not increase the possibility to induce resistant strains in intestinal microflora.
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