Easton C J, Knowles J R
Antimicrob Agents Chemother. 1984 Sep;26(3):358-63. doi: 10.1128/AAC.26.3.358.
The effectiveness of clavulanic acid, sulbactam, quinacillin sulfone, and the carbapenems MM13902 and MM4550 as inhibitors of TEM-2 beta-lactamase in growing cultures of gram-negative bacteria has been studied. Each of these beta-lactams inhibited the enzyme in intact cells, and the nature of the inhibition correlated with studies on the purified enzyme. The potency of these compounds as inhibitors of the beta-lactamase in vivo can be correlated with the amounts hydrolyzed by the purified enzyme under saturating conditions during the inhibition of the enzyme in vitro.
已对克拉维酸、舒巴坦、喹那西林砜以及碳青霉烯类药物MM13902和MM4550作为革兰氏阴性菌生长培养物中TEM-2β-内酰胺酶抑制剂的有效性进行了研究。这些β-内酰胺类药物中的每一种都能在完整细胞中抑制该酶,且抑制的性质与对纯化酶的研究相关。这些化合物作为体内β-内酰胺酶抑制剂的效力可与在体外抑制该酶期间,纯化酶在饱和条件下所水解的量相关联。