齐德巴坦（Zidebactam） 更新时间：2021-05-13 09:40:33 常用名 齐特巴坦 CAS号 1436861-97-0 价钱 ￥需询单/100mg ￥需询单/1g 纯度 98.0% 备货期 需询单 库存 询单 产物详情（用途，包装等） Zidebactam and WCK 5153 are novel β-lactam enhancers that are bicyclo-acyl hydrazides (BCH), derivatives of the diazabicyclooctane (DBO) scaffold, targeted for the treatment of serious infections caused by highly drug-resistant Gram-negative pathogens. In this study, we determined the penicillin-binding protein (PBP) inhibition profiles and the antimicrobial activities of zidebactam and WCK 5153 against Pseudomonas aeruginosa, including multidrug-resistant (MDR) metallo-β-lactamase (MBL)-producing high-risk clones. MIC determinations and time-kill assays were conducted for zidebactam, WCK 5153, and antipseudomonal β-lactams using wild-type PAO1, MexAB-OprM-hyperproducing (mexR), porin-deficient (oprD), and AmpC-hyperproducing (dacB) derivatives of PAO1, and MBL-expressing clinical strains ST175 (blaVIM-2) and ST111 (blaVIM-1). Furthermore, steady-state kinetics was used to assess the inhibitory potential of these compounds against the purified VIM-2 MBL. Zidebactam and WCK 5153 showed specific PBP2 inhibition and did not inhibit VIM-2 (apparent Ki [Kiapp] > 100 μM). MICs for zidebactam and WCK 5153 ranged from 2 to 32 μg/ml (amdinocillin MICs > 32 μg/ml). Time-kill assays revealed bactericidal activity of zidebactam and WCK 5153. LIVE-DEAD staining further supported the bactericidal activity of both compounds, showing spheroplast formation. Fixed concentrations (4 or 8 μg/ml) of zidebactam and WCK 5153 restored susceptibility to all of the tested β-lactams for each of the P. aeruginosa mutant strains. Likewise, antipseudomonal β-lactams (CLSI breakpoints), in combination with 4 or 8 μg/ml of zidebactam or WCK 5153, resulted in enhanced killing. Certain combinations determined full bacterial eradication, even with MDR MBL-producing high-risk clones. β-Lactam–WCK enhancer combinations represent a promising β-lactam “enhancer-based” approach to treat MDR P. aeruginosa infections, bypassing the need for MBL inhibition. 供应商信息 河北唯特医药科技有限公司 认证状态： 未认证供应商 电话： 13180081292 地址： 河北省石家庄市裕华区育才街251号 区域： 河北省 石家庄市 裕华区 联系人： 王司理 联系人电话： 13180081292 邮件： wetogethermeditech@163.com 主要市场： 中国大陆，日本，印度 年商业额： 100w 河北唯特医药科技有限公司专注于抗生素增强剂（Antibiotic enhancer）的研发和生产，尤其以β内酰胺酶抑制剂类管线的药物为营业主线，提供阿维巴坦（Avibactam），瑞莱巴坦（Relebactam），齐德巴坦（Zidebactam），法硼巴坦（Vaborbactam），WCK-5153，等一系列β内酰胺酶抑制剂的API, 中央体，杂质，研发生产，手艺服务和手艺转让列服务。