更新于：2024-12-09
Enoxacin
依诺沙星
更新于：2024-12-09
概要
基本信息
药物类型 小分子化药 |
别名 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic acid、1-Ethyl-6-fluoro-4-oxo-7-piperazin-1-yl-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid、Enoxacin (USAN/INN) + [39] |
作用机制 细菌DNA旋转酶复合体抑制剂、Bacterial Top II抑制剂(细菌拓扑异构酶II抑制剂)、Bacterial top IV抑制剂(细菌拓扑异构酶IV抑制剂) |
治疗领域 |
在研适应症 |
非在研适应症- |
原研机构 |
在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (1991-12-31), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (欧盟) |
登录后查看时间轴
结构
分子式C15H17FN4O3 |
InChIKeyIDYZIJYBMGIQMJ-UHFFFAOYSA-N |
CAS号74011-58-8 |
关联
1
项与 依诺沙星 相关的临床试验A Randomized, Double-blind, Parallel Group, Single Centre, Phase 1b/2 Study to Assess the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Three Orally Administered Doses of Enoxacin (200mg Twice Daily, 400mg Twice Daily and 600mg Twice Daily) in Adults With Amyotrophic Lateral Sclerosis
100 项与 依诺沙星 相关的临床结果
登录后查看更多信息
100 项与 依诺沙星 相关的转化医学
登录后查看更多信息
100 项与 依诺沙星 相关的专利（医药）
登录后查看更多信息
1,124
项与 依诺沙星 相关的文献（医药）2024-12-20Journal of biomolecular structure & dynamics
Computational insights into VacA toxin inhibition: harnessing FDA-approved antibiotics against
Helicobacter pylori
Article
作者: Saini, Vaishali ; Jha, Hem Chandra ; Varshney, Nidhi ; Samanta, Sunanda ; Roy, Rajarshi ; Koirala, Suman ; Kashyap, Dharmendra ; Bagde, Pranit Hemant ; Kar, Parimal
Cancer is a condition in which a few of the body's cells grow beyond its control and spread to other outward regions. Globally, gastric cancer (GC) is third most common cause of cancer-related mortality and the fourth most common kind of cancer. Persistent infection of VacA-positive Helicobacter pylori (H. pylori) modulates cellular physiology and leads to GC. About ∼70% of H. pylori are positive for vacuolating cytotoxin-A (VacA), and it infects ∼80-90% of world populations. Herein, for first time, we repurposed FDA-approved gram-negative antibiotics, which are feasible alternatives to existing regimens and may be used in combinatorial treatment against VacA-positive H. pylori. Out of 110 FDA-approved antibiotics, we retrieved 92 structures, which were screened against the VacA protein. Moreover, we determined that the top eight hit antibiotics viz; cefpiramide, cefiderocol, eravacycline, doxycycline, ceftriaxone, enoxacin, tedizolid, and cefamandole show binding free energies of -9.1, -8.9, -8.1, -8.0, -7.9, -7.8, -7.8 and -7.8 Kcal/mol, respectively, with VacA protein. Finally, we performed 100 ns duplicate MD simulations on the top eight selected antibiotics showing strong VacA binding. Subsequently, five antibiotics, including cefiderocol, cefpiramide, doxycycline, enoxacin, and tedizolid show stable ligand protein distance and good binding affinity revealed by the MM-PBSA scheme. Among the five antibiotics cefiderocol act as the most potent inhibitor (-28.33 kcal/mol). Furthermore, we also identified the hotspot residue like Asn-506, Tyr-529, and Phe-483 which control the interaction. Concisely, we identified antibiotics that can be repurposed against VacA of H. pylori and explored their molecular mechanism of interaction with VacA.Communicated by Ramaswamy H. Sarma.
2024-12-01ENVIRONMENTAL POLLUTION
Toxicological mechanisms and molecular impacts of tire particles and antibiotics on zebrafish
Article
作者: Li, Tong ; Fenech, Adam ; Wen, Jingya ; Gao, Jiaxuan ; Pu, Qikun ; Li, Yu ; Ding, Xiaowen ; Liu, Yajing
Tire microplastics (TMPs) and antibiotics are emerging pollutants that widely exist in water environments. The coexistence of these pollutants poses severe threats to aquatic organisms. However, the toxicity characteristics and key molecular factors of the combined exposure to TMPs in aquatic organisms remain unknown. Therefore, the joint toxicity of styrene-butadiene rubber TMPs (SBR-TMPs) and 32 antibiotics (macrolides, fluoroquinolones, β-lactams, sulfonamides, tetracyclines, nitroimidazoles, highly toxic antibiotics, high-content antibiotics, and common antibiotics) in zebrafish was investigated using a full factorial design, molecular docking, and molecular dynamics simulation. Sixty-four combinations of antibiotics were designed to investigate the hepatotoxicity of the coexistence of SBR-TMPs additives and antibiotics in zebrafish. Results indicated that low-order effects of antibiotics (e.g., enoxacin-lomefloxacin and ofloxacin-enoxacin-lomefloxacin) had relatively notable toxicity. The van der Waals interaction between additives and zebrafish cytochrome P450 enzymes primarily affected zebrafish hepatotoxicity. Zebrafish hepatotoxicity was also affected by the ability of SBR-TMPs to adsorb antibiotics, the relation between antibiotics, the affinity of antibiotics docking to zebrafish cytochrome P450 enzymes, electronegativity, atomic mass, and the hydrophobicity of the antibiotic molecules. This study aimed to eliminate the joint toxicity of TMPs and antibiotics and provide more environmentally friendly instructions for using different chemicals.
2024-08-01CHEMOSPHERE
Distribution and ecological risk assessment of antibiotics in different freshwater aquaculture ponds in a typical agricultural plain, China
Article
作者: Zhang, Lu ; Li, Yong ; Wei, Huimin ; Wang, Cong ; Cheng, Yiting ; Wang, Zhi
Freshwater aquaculture serves as a significant focal point for antibiotic contamination, yet understanding antibiotic distribution across different aquaculture models and stages remains limited. This study evaluated antibiotic pollution in three distinct freshwater aquaculture models: rice-crayfish coculture, fish aquaculture, and crab-crayfish aquaculture, during various aquaculture stages. Of the 33 target antibiotics, 16 antibiotics were detected, with the total concentrations ranging from 111.81 ng/L to 15,949.05 ng/L in water and 10.11 ng/g to 8986.30 ng/g in sediment. Among these antibiotics, erythromycin and lomefloxacin are prohibited for use in Chinese aquaculture. Dominant antibiotics in water included lincomycin, enrofloxacin, and enoxacin, whereas in sediment, oxytetracycline and erythromycin were predominant. Notably, lincomycin emerged as a dominant antibiotic in aquaculture for the first time. The concentrations of these dominant antibiotics were high compared to other aquaculture settings and exhibited elevated ecological risk. Critical periods for antibiotic contamination in water and sediment were found to be incongruent, occurring during the rainy season in July for water and the dry season in October for sediment. Notably, the rice-crayfish coculture model exerts a good effect in reducing antibiotic pollution. Overall, these findings offer valuable evidence for the healthful and sustainable advancement of aquaculture.
100 项与 依诺沙星 相关的药物交易
登录后查看更多信息
研发状态
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 细菌感染 | 美国 | 1991-12-31 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
来和芽仔聊天吧
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用