Impurity Identification and Scale-Up of a Novel Glycopeptide Antibiotic
文献类型：期刊论文
| 作者 | Jiao, Shang1,2; Guan, Dongliang3; Xu, Lili1,2; Liu, Bo4; Shi, Weiwei1,2; Li, Jian1,2; Tang, Feng1,2; Huang, Wei1,2,4 |
| 刊名 | ORGANIC PROCESS RESEARCH & DEVELOPMENT
 |
| 出版日期 | 2021-11-19 |
| 卷号 | 25期号:11页码:2390-2402 |
| 关键词 | glycopeptide antibiotics impurity analytical method process optimization and development |
| ISSN号 | 1083-6160 |
| DOI | 10.1021/acs.oprd.1c00064 |
| 通讯作者 | Tang, Feng(tangfeng2013@simm.ac.cn) ; Huang, Wei(huangwei@simm.ac.cn) |
| 英文摘要 | A variety of novel glycopeptide antibiotics have been developed to combat the drug-resistant bacterial strains. Previously, we reported a series of vancomycin derivatives that are modified with lipid tails and extra sugars. SM-V-61, as one of the vancomycin analogues with a trifluoromethyl-biphenyl fragment and galactose, showed enhanced antibacterial activity, improved PK/PD, better water solubility, and safety. However, the deficient synthetic procedure, lower yield, and complicated impurities hindered the further development of the drug candidate SM-V-61. Herein, we reported a further study on SM-V-61 impurity analysis and process optimization. We first synthesized and identified a variety of impurities and established the analytical method for quality analysis and control of SM-V-61. Based on the defined analytical method, we optimized the synthetic procedure for SM-V-61 and operated the synthesis on 30-40 and 500-600 g scales in the laboratory and manufacturing workshop, respectively. |
| WOS关键词 | VANCOMYCIN ; DIMERIZATION ; RETENTION ; PH |
| 资助项目 | National Natural Science Foundation of China (NNSFC)[21877116] ; SIMM Institute Fund[CASIMM0120202009] ; Shanghai Action Plan of Technological Innovation[18431900700] ; National Mega-Project for Innovative Drugs[2019ZX09721001-004-009] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000726748300002 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/299220]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Tang, Feng; Huang, Wei |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Biotherapeut Discovery Res, CAS Key Lab Receptor Res,CAS Ctr Excellence Mol C, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Res Triangle Inst, Ctr Drug Discovery, Res Triangle Pk, NC 27709 USA 4.Univ Chinese Acad Sci, Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310024, Peoples R China |
| 推荐引用方式 GB/T 7714 | Jiao, Shang,Guan, Dongliang,Xu, Lili,et al. Impurity Identification and Scale-Up of a Novel Glycopeptide Antibiotic[J]. ORGANIC PROCESS RESEARCH & DEVELOPMENT,2021,25(11):2390-2402. |
| APA | Jiao, Shang.,Guan, Dongliang.,Xu, Lili.,Liu, Bo.,Shi, Weiwei.,...&Huang, Wei.(2021).Impurity Identification and Scale-Up of a Novel Glycopeptide Antibiotic.ORGANIC PROCESS RESEARCH & DEVELOPMENT,25(11),2390-2402. |
| MLA | Jiao, Shang,et al."Impurity Identification and Scale-Up of a Novel Glycopeptide Antibiotic".ORGANIC PROCESS RESEARCH & DEVELOPMENT 25.11(2021):2390-2402. |
入库方式： OAI收割
来源：上海药物研究所
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