Kuck N A, Petersen P J, Weiss W J, Testa R T
American Cyanamid Co., Medical Research Division, Pearl River, NY 10965.
J Chemother. 1989 Jun;1(3):155-61. doi: 10.1080/1120009x.1989.11738884.
YTR-830H, a beta-lactamase inhibitor, is a non-amino penicillanic sulfone. In vitro synergistic activity with piperacillin was determined for 226 beta-lactamase producing clinical cultures. Combination of piperacillin: YTR in ratios of 2:1, 4:1, and 8:1 were highly effective vs Escherichia coli, Proteus, Providencia, Morganella, Staphylococcus, and Bacteroides. Minimum inhibitory concentrations (MICs) of piperacillin were reduced from the resistant to susceptible range. The higher ratios were less effective vs Enterobacter, Serratia, and Citrobacter. YTR-830H was not antagonistic with piperacillin. Combinations of 2:1, 4:1, and 8:1 increased the therapeutic effectiveness of piperacillin 8 - to 36 - fold against acute lethal infections produced in mice with piperacillin-resistant Escherichia coli, Klebsiella pneumoniae, Morganella morganii, and Staphylococcus aureus.
YTR - 830H是一种β - 内酰胺酶抑制剂，属于非氨基青霉烷砜。对226株产β - 内酰胺酶的临床培养菌株测定了其与哌拉西林的体外协同活性。哌拉西林与YTR以2:1、4:1和8:1的比例联合使用时，对大肠杆菌、变形杆菌、普罗威登斯菌、摩根菌、葡萄球菌和拟杆菌具有高效性。哌拉西林的最低抑菌浓度（MICs）从耐药范围降至敏感范围。较高比例对肠杆菌、沙雷菌和柠檬酸杆菌的效果较差。YTR - 830H与哌拉西林无拮抗作用。2:1、4:1和8:1的联合用药使哌拉西林对小鼠由耐哌拉西林的大肠杆菌、肺炎克雷伯菌、摩根摩根菌和金黄色葡萄球菌引起的急性致死性感染的治疗效果提高了8至36倍。
