三唑巴坦对β-内酰胺酶抑制作用的研究进展  

Development in Studies of Inhibition of Tazobactam Against β-lactamaes

作　　者：陈昭丽[1,2] 王霆 李苌清 张兴艳[1,2] 程泽能[1] 

机构地区：[1]中南大学药学院药物分析教研室,长沙410013 [2]湘北威尔曼制药有限公司,长沙410000

出　　处：《国外医药（抗生素分册）》2010年第4期184-189,共6页World Notes on Antibiotics

摘　　要：三唑巴坦是第三个上市的β-内酰胺酶抑制剂,具有抑酶活性强,抑酶谱广等特点,对绝大多数A类β-内酰胺酶有较强的抑制作用,对C类和D类β-内酰胺酶也有一定的的抑制作用。因此,三唑巴坦在临床产酶耐药菌所致感染性疾病的治疗中具有重要作用。但不可忽视的是,三唑巴坦上市20余年来已有30余种耐三唑巴坦的耐酶抑制剂β-内酰胺酶在欧美国家出现,而对三唑巴坦敏感性较差的β类酶在我国也有报道,这些酶的出现和流行将严重威胁三唑巴坦在临床中的使用。本文将三唑巴坦抑酶作用的分子机制、对各类β-内酰胺酶的抑制作用以及耐酶抑制剂与β-内酰胺酶的构效关系作一综述。Tazobactam, a β-lactamase inhibitor, has a strong and an excellent spectrum inhibitory activity against a large variety of β-lactamase, which could effectively inhibit Class A, C class and D class β - lactamases. Therefore, tazobactam plays an important part in the treatment of clinical infectious diseases by β-lactamase-producing strains, But it is noteworthy that more than 30 kinds of Inhibitor-resistant beta-lactamases （IRBLs） found in European and American countries and tazobactam-resistant beta-lactamases also reported in china posed a serious threat to the continued use of tazobactam in the clinical. To better understand the inhibition of tazobactam, the molecular mechanism of inhibition inhibitory activity against four types of beta-lactamases and the structure-activity relationships of IRBLs were reviewed in this oaoer.

关 键 词：三唑巴坦 Β-内酰胺酶 IRBLs 半数抑菌浓度(IC50) 抑制常数(Ki) 

分 类 号：R978.11[医药卫生—药品]