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齐德巴坦

(2S,5R)-7-oxo-6-(sulfooxy)-1,6-diazabicyclo[3.2.1] octane-2-carboxylic acid, 2-[2-[(3R)-3-piperidinylcarbonyl]hydrazide ]
1436861-97-0
9000 1g 起订
询价 5g 起订
询价 10g 起订
河北 更新日期:2025-01-02

河北唯特医药科技有限公司

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联系人:王经理
手机:13180081292 拨打
邮箱:contact@wetogethermed.com

产品详情:

中文名称:
齐德巴坦
英文名称:
(2S,5R)-7-oxo-6-(sulfooxy)-1,6-diazabicyclo[3.2.1] octane-2-carboxylic acid, 2-[2-[(3R)-3-piperidinylcarbonyl]hydrazide ]
CAS号:
1436861-97-0
纯度规格:
≥98% HPLC
产品类别:
β内酰胺酶抑制剂
自定义货号:
WTM-001--00

cas号:1436861-97-0

分子式:C13H21N5O7S

分子量:391.4001

中文别名:Zidebactam

英文别名:(1R,2S,5R)-7-oxo-2-(2-((R)-piperidine-3-carbonyl)hydrazine-1-carbonyl)-1,6-diazabicyclo[3.2.1]octan-6-yl hydrogen sulfate,WCK-5107,Zidebactam,YPM97423DB,[(2S,5R)-7-oxo-2-[[[(3R)-piperidine-3-carbonyl]amino]carbamoyl]-1,6-diazabicyclo[3.2.1]octan-6-yl] hydrogen sulfate,Zidebactam [INN],Zidebactam, (-)-,GTPL10874


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.


zidebactam ;齐德巴坦;齐达巴坦;WCK 5107;1436861-97-0 ;

公司简介

河北唯特医药科技有限公司专注于苯并杂环Block,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业务主线,提供阿维巴坦(Avibactam),瑞莱巴坦(Relebactam),齐德巴坦(Zidebactam),WCK-5153,等一系列β内酰胺酶抑制剂的中间体,API的研发生产,技术服务和技术转让等一系列服务。

成立日期 (5年)
注册资本 300万人民币
员工人数 1-10人
年营业额 ¥ 100万-300万
经营模式 工厂,定制
主营行业 医药中间体,有机合成药,青霉素类,头孢菌素类,其他西药原料

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