Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability
文献类型：期刊论文
| 作者 | Liu, Yu; Liu, Zining; Cao, Xufeng; Liu, Xin; He, Huili; Yang, Yushe
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2011-08-15 |
| 卷号 | 21期号:16页码:4779-4783 |
| 关键词 | Itraconazole analogues Synthesis Antifungal Bioavailability |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2011.06.062 |
| 文献子类 | Article |
| 英文摘要 | To improve antifungal activities, water solubility and bioavailability, a series of novel analogues of itraconazole-containing pyridine rings were designed and synthesized. Their antifungal activities were evaluated in vitro against six clinically important fungi by measuring the minimal inhibitory concentrations (MICs). Most of the compounds showed more potent antifungal activities than that of itraconazole. In particular, the analogues 30d, 30c, 31c, and 36d exhibited much higher solubility and bioavailability than that of itraconazole. The bioavailability of 36d (42.2%) was five times higher than that of itraconazole (8%) and was negative for genetic toxicology in the Ames test. (C) 2011 Published by Elsevier Ltd. |
| WOS关键词 | BROAD-SPECTRUM ANTIFUNGAL ; SURVEILLANCE ; POSACONAZOLE ; AZOLE |
| 资助项目 | Key New Drug Creation and Manufacturing Program, China[2009ZX09301-001] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000293168000024 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278438]  |
| 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, Yushe |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Yu,Liu, Zining,Cao, Xufeng,et al. Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2011,21(16):4779-4783. |
| APA | Liu, Yu,Liu, Zining,Cao, Xufeng,Liu, Xin,He, Huili,&Yang, Yushe.(2011).Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,21(16),4779-4783. |
| MLA | Liu, Yu,et al."Design and synthesis of pyridine-substituted itraconazole analogues with improved antifungal activities, water solubility and bioavailability".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 21.16(2011):4779-4783. |
入库方式： OAI收割
来源：上海药物研究所
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