更新于：2024-12-14
Cephradine
头孢拉定
更新于：2024-12-14
概要
基本信息
药物类型 小分子化药 |
别名 (6R,7R)-7-((R)-2-Amino-2-(1,4-cyclohexadien-1-yl)acetamido)-3-methyl-8-oxo-5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid、(6R,7R)-7-{[(2R)-2-amino-2-cyclohexa-1,4-dien-1-ylacetyl]amino}-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid、7-(D-2-Amino-2-(1,4-cyclohexadienyl)acetamide)desacetoxycephalosporanicacid + [19] |
靶点 |
作用机制 PBPs抑制剂(细菌青霉素结合蛋白家族抑制剂)、细胞壁抑制剂 |
治疗领域 |
在研适应症 |
在研机构 |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C16H19N3O4S |
InChIKeyRDLPVSKMFDYCOR-UEKVPHQBSA-N |
CAS号38821-53-3 |
关联
26
项与 头孢拉定 相关的临床试验Oral Versus Intravenous Antibiotic Prophylaxis Before Obstetric and Gynecological Procedures
头孢拉定胶囊在中国健康受试者中单中心、随机、开放、单剂量、两周期交叉空腹及餐后状态下的生物等效性试验
头孢拉定胶囊（0.25g/粒）在中国健康受试者中空腹和餐后给药条件下随机、开放、单剂量、两序列、两周期、双交叉生物等效性试验
100 项与 头孢拉定 相关的临床结果
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100 项与 头孢拉定 相关的转化医学
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100 项与 头孢拉定 相关的专利（医药）
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902
项与 头孢拉定 相关的文献（医药）2024-12-11JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
Production of Natural Penicillin-Binding Protein 2 and Development of a Signal-Amplified Fluorescence Polarization Assay for the Determination of 28 Beta-Lactam Antibiotics in Milk
Article
作者: Hu, Jia Jia ; Wang, Jian Ping
In this study, two magnetic activity-based protein profiling probes based on cephradine and amoxicillin were first synthesized that were used to produce the natural penicillin-binding protein 2 of Escherichia coli. After characterization by using LC-ESI-MS/MS, it was found that the obtained proteins by using the two probes were the same. The molecular docking for 28 beta-lactam antibiotics showed that the key amino acids were Ser330 and Ser387, the main intermolecular forces were hydrogen bond and hydrophobic interaction, and the main binding sites in their molecules were on the beta-lactam ring. Then this protein was combined with streptavidin-labeled tracer and biotinylated fluorescein isothiocyanate to establish a signal-amplified fluorescence polarization assay to determine the 28 drugs in milk. The limits of detection ranged from 0.07 to 2.21 ng/mL, and the sensitivities for the 28 drugs were improved 4 to 48-fold in comparison with the use of a fluorescein isothiocyanate-labeled fluorescent tracer. Therefore, this method could be used for rapid multiscreening of the 28 beta-lactam antibiotics in milk.
2024-12-01YAKUGAKU ZASSHI-JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN
Analysis of Endogenous Metabolite Transporters for the Development of Novel Pharmaceutical Therapies and Drug Targets
Review
作者: Higuchi, Kei
Transporters are critical for maintaining the homeostasis of metabolites within cells, organelles, and extracellular fluids. Various transporters have been targeted for development as pharmaceutical therapies, including glucose transporter (SLC5A2/SGLT2) and urate transporter (SLC22A12/URAT1). The solute carrier transporter family includes many orphan transporters with unknown physiological functions and substrates, largely because of the difficulties in optimizing the transporter probes and constructing convenient evaluation systems for functional analysis. However, the analysis of these transporters is important as they may be potential candidates for pharmaceutical therapies or drug targets. This review focuses on the analysis of the SLC16A family, which encodes monocarboxylate transporters (MCTs), as it contains orphan transporters known to be associated with several disease pathologies. We successfully identified taurine, cephradine, and 5-carboxyfluorescein as new substrates for rat Slc16a6/MCT7, SLC16A13/MCT13, and SLC16A5/MCT6, respectively. These substrates enabled the functional analysis of the transporters in mammalian cells. We found that the co-expression of ancillary proteins, such as ancillary protein basigin/CD147 and embigin/GP70, enhanced the transport functions of these transporters. Interestingly, the functions of MCT6 and MCT13 were affected by extracellular chloride and potassium ions, respectively, but MCT7 was unaffected. These findings are helpful for elucidating the pathophysiological roles and substrates of orphan and uncharacterized MCTs.
2024-11-01SCIENCE OF THE TOTAL ENVIRONMENT
Adsorption mechanism of cefradine on three microplastics: A combined molecular dynamics simulation and density functional theory calculation study
Article
Microplastics and antibiotics are receiving increasing attention as two emerging pollutants in the aquatic ecosystem. The absorption of antibiotics by microplastics can potentially intensify their impact on marine organisms and human health. However, the detailed mechanisms underlying this interaction remain to be elucidated. Through molecular dynamics (MD) simulations and density functional theory (DFT) calculations, this study investigated the adsorption of cefradine (CED) onto three typical microplastics (MPs)-polyethylene (PE), polypropylene (PP), and polyamide (PA). The results of the molecular dynamics simulations showed that the interaction energy between CED and microplastics followed the order of PA-CED > PP-CED > PE-CED, indicating that PA microplastics had the highest adsorption capacity for CED antibiotics. The total energy contribution of the microplastics-cefradine (MPs-CED) systems suggested that the van der Waals and electrostatic interactions were the two primary mechanisms for the adsorption of CED by these three microplastics. In DFT calculations, the adsorption of CED on PA was found to be significantly influenced by both electrostatic and van der Waals effects, while the main driving force in the adsorption of PE and PP is van der Waals effect. In addition, IGMH analysis and AIM topological analysis confirmed that the adsorption of CED on PA relied heavily on the synergistic effect of hydrogen bonding and the van der Waals effect. The findings of this study validate the results obtained from molecular dynamics simulations, laying a foundation for a comprehensive exploration of the interaction mechanisms between microplastics and organic pollutants by integrating MD simulations and DFT calculations.
100 项与 头孢拉定 相关的药物交易
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研发状态
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 细菌感染 | 中国 | 1985-01-01 | |
| 革兰氏阴性菌感染 | 美国 | 1982-01-01 | |
| 革兰氏阳性细菌感染 | 美国 | 1982-01-01 |
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