Synthesis, pharmacokinetics and in vivo antifungal activity of the novel water-soluble prodrugs of itraconazole analogue YL-24
文献类型：期刊论文
| 作者 | Liu, Yu2; Cao, Xu-Feng2; Liu, Xin2; Cao, Yong-Bing1; Chu, Wen-Jing2; Yang, Yu-She2
|
| 刊名 | CHINESE CHEMICAL LETTERS
 |
| 出版日期 | 2013-04 |
| 卷号 | 24期号:4页码:321-324 |
| 关键词 | Synthesis Antifungal Water-soluble prodrugs Itraconazole analogue |
| ISSN号 | 1001-8417 |
| DOI | 10.1016/j.cclet.2013.03.008 |
| 文献子类 | Article |
| 英文摘要 | To improve the aqueous solubility of an itraconazole analogue, compound 1 (YL-24), a series of novel prodrugs were synthesized. Among these prodrugs, the phosphate disodium salt compound 7 exhibited excellent aqueous solubility (9.8 mg/mL) at near-neutral pH and sufficient stability in buffer solutions, along with favorable pharmacokinetic profiles. In particular, compounds 1 and 7 provided moderate survival efficacy in murine systemic Candida albicans SC5314 infection model, but their efficacy was weaker than that of fluconazole. (C) 2013 Yu-She Yang. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved. |
| WOS关键词 | DERIVATIVES ; SPECTRUM ; DESIGN ; AGENT |
| 资助项目 | National Science and Technology Major Project[00000000] ; Key New Drug Creation and Manufacturing Program, China[2009ZX09301-001] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| CSCD记录号 | CSCD:4840474 |
| WOS记录号 | WOS:000319307900015 |
| 出版者 | ELSEVIER SCIENCE INC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277664]  |
| 专题 | 药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Yang, Yu-She |
| 作者单位 | 1.Second Mil Med Univ, Sch Pharm, Shanghai 200433, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 20103, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Liu, Yu,Cao, Xu-Feng,Liu, Xin,et al. Synthesis, pharmacokinetics and in vivo antifungal activity of the novel water-soluble prodrugs of itraconazole analogue YL-24[J]. CHINESE CHEMICAL LETTERS,2013,24(4):321-324. |
| APA | Liu, Yu,Cao, Xu-Feng,Liu, Xin,Cao, Yong-Bing,Chu, Wen-Jing,&Yang, Yu-She.(2013).Synthesis, pharmacokinetics and in vivo antifungal activity of the novel water-soluble prodrugs of itraconazole analogue YL-24.CHINESE CHEMICAL LETTERS,24(4),321-324. |
| MLA | Liu, Yu,et al."Synthesis, pharmacokinetics and in vivo antifungal activity of the novel water-soluble prodrugs of itraconazole analogue YL-24".CHINESE CHEMICAL LETTERS 24.4(2013):321-324. |
入库方式： OAI收割
来源：上海药物研究所
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