PZ0014
利奈唑胺
≥98% (HPLC), powder, bacterial mRNA translation inhibitor
别名:
N-[[（5S）-3-[3-氟-4-（4-吗啉基）苯基] -2-氧代-5-恶唑烷基]甲基]乙酰胺, PNU-100766, U-100766
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关于此项目
经验公式（希尔记法）:
C16H20FN3O4
化学文摘社编号:
分子量:
337.35
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
产品名称
利奈唑胺, ≥98% (HPLC)
方案
≥98% (HPLC)
表单
powder
颜色
white to off-white
溶解性
DMSO: >20 mg/mL
储存温度
room temp
SMILES字符串
CC(=O)NC[C@H]1CN(C(=O)O1)c2ccc(N3CCOCC3)c(F)c2
InChI
1S/C16H20FN3O4/c1-11(21)18-9-13-10-20(16(22)24-13)12-2-3-15(14(17)8-12)19-4-6-23-7-5-19/h2-3,8,13H,4-7,9-10H2,1H3,(H,18,21)/t13-/m0/s1
InChI key
TYZROVQLWOKYKF-ZDUSSCGKSA-N
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一般描述
利奈唑胺对多种革兰氏阳性菌具有抗菌活性，包括耐青霉素菌、耐甲氧西林菌和耐万古霉素菌。利奈唑胺可通过抑制起始复合物形成降低翻译反应速率，从而缩短新合成肽链长度。此外，它还有减少毒力因子的作用，可减少革兰氏阳性菌产生的毒素。
应用
利奈唑胺已用于棋盘式药物组合 MIC（最小抑制浓度）检测，以确定 ivacaftor是否与利奈唑胺的具有正相互作用。 已用于测定最低生物膜抑制浓度和用于治疗脓肿分枝杆菌感染的黑腹果蝇w1118。利奈唑胺已作为抗生素，研究它对大鼠肺部疟疾相关呼吸窘迫综合征(MAARDS)发生发展的影响。作为抗生素与黄苓素联用，研究它对耐甲氧西林金黄色葡萄球菌株的影响。作为抗生素，研究它对浮游生物生长和粪肠球菌生物膜形成的影响。
生化/生理作用
利奈唑胺是一种恶唑烷类抗菌药。它抑制细菌 mRNA的翻译和是一种弱的、可逆的、非选择性的单胺氧化酶抑制剂。
利奈唑胺是一种恶唑烷酮类抗菌药。 它与50S 亚基的细菌 23S 核糖体 RNA 上的位点结合，并阻止功能性 70S 起始复合物的形成，从而抑制细菌 mRNA 翻译。利奈唑胺也是一种弱的、可逆的非选择性单胺氧化酶抑制剂。
警示用语：
Danger
危险声明
危险分类
STOT RE 1 Oral
靶器官
Bone
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Seyed Mohammad Reza Hashemian et al.
Drug design, development and therapy, 12, 1759-1767 (2018-06-29)
Linezolid can be considered as the first member of the class of oxazolidinone antibiotics. The compound is a synthetic antibiotic that inhibits bacterial protein synthesis through binding to rRNA. It also inhibits the creation of the initiation complex during protein
Laura Morata et al.
Antimicrobial agents and chemotherapy, 57(4), 1913-1917 (2013-02-14)
Linezolid is an antibiotic with time-dependent activity, and both the percentage of time that plasma concentrations exceed the MIC and the area under the concentration-time curve over 24 h in the steady state divided by the MIC (AUC24/MIC ratio) are
Zhong Chen et al.
Journal of medicinal chemistry, 64(20), 15037-15052 (2021-10-19)
YycFG, one of the two-component systems involved in the regulation of biofilm formation, has attracted increasing interest as a potential target of antibacterial and antibiofilm agents. YycG inhibitors for Staphylococcus aureus and Staphylococcus epidermidis have been developed, but Enterococcus faecalis
Giovanni Sotgiu et al.
The European respiratory journal, 40(6), 1430-1442 (2012-04-13)
Linezolid is used off-label to treat multidrug-resistant tuberculosis (MDR-TB) in absence of systematic evidence. We performed a systematic review and meta-analysis on efficacy, safety and tolerability of linezolid-containing regimes based on individual data analysis. 12 studies (11 countries from three
Gregory J Moran et al.
The Lancet. Infectious diseases, 14(8), 696-705 (2014-06-10)
New antibiotics are needed to treat infections caused by drug-resistant bacteria. Tedizolid is a novel oxazolidinone antibacterial drug designed to provide enhanced activity against Gram-positive pathogens. We aimed to assess the efficacy and safety of intravenous to oral tedizolid for
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Bioactive small molecules for immune system signaling target identification/validation and antibiotics, antivirals, and antifungals offered.
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