Application of Sulfonyl in Drug Design
文献类型：期刊论文
| 作者 | Zhao Fei1,2; Wang Jiang1 ; Ding Xiao1; Shu Shuangjie1; Liu Hong1
|
| 刊名 | CHINESE JOURNAL OF ORGANIC CHEMISTRY
 |
| 出版日期 | 2016-03 |
| 卷号 | 36期号:3页码:490-501 |
| 关键词 | sulfonyl drug design lead optimization |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc201510006 |
| 文献子类 | Review |
| 英文摘要 | Sulfonyl-containing compounds comprise a substantial proportion in the therapeutic drugs. It is an important strategy to introduce sulfonyl group into the small molecules for structure-based medicinal chemistry, the application of sulfonyl group in drug design is reviewed in this paper. Structurally, sulfonyl group has similar properties in molecular size and charge distribution with carbonyl, carboxyl, tetrazolium and phosphate group, so it can be introduced into the drug molecules as their bioisostere in order to remain or improve activity. Sulfonyl group possesses unique physicochemical properties, and the introduction of sulfonyl group can also modulate the solubility and acid-base property of the drug molecules. Sulfonyl group can offer two hydrogen-bond receptors, and reasonable introduction of sulfonyl group can enhance the binding affinity of the drug molecules with the targeted proteins to improve activity through hydrogen bond interactions. What's more, sulfonyl group is relatively stable in terms of structure, the introduction of sulfonyl group can increase the metabolic stability of drugs to prolong the duration of action by blocking metabolically labile sites, improve the pharmacokinetic properties of the drug molecules to elevate the bioavailability. Sulfonyl group belongs to polar groups, which can also increase the polarity of the drug molecules to diminish hERG activity. |
| WOS关键词 | RECEPTOR ANTAGONIST ; ANGIOTENSIN-II ; POTENT ; DISCOVERY ; INHIBITORS ; DERIVATIVES ; AGENTS ; ANALOGS ; BINDING ; SERIES |
| 资助项目 | National Natural Science Foundation of China[21372235] |
| WOS研究方向 | Chemistry |
| 语种 | 中文 |
| CSCD记录号 | CSCD:5684271 |
| WOS记录号 | WOS:000375637600005 |
| 出版者 | SCIENCE PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276108]  |
| 专题 | 药物化学研究室 |
| 通讯作者 | Liu Hong |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Key Lab Receptor Res, Shanghai 201203, Peoples R China; 2.Chengdu Univ, Sichuan Ind Inst Antibiot, Antibiot Res & Reevaluat Key Lab Sichuan Prov, Chengdu 610052, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhao Fei,Wang Jiang,Ding Xiao,et al. Application of Sulfonyl in Drug Design[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2016,36(3):490-501. |
| APA | Zhao Fei,Wang Jiang,Ding Xiao,Shu Shuangjie,&Liu Hong.(2016).Application of Sulfonyl in Drug Design.CHINESE JOURNAL OF ORGANIC CHEMISTRY,36(3),490-501. |
| MLA | Zhao Fei,et al."Application of Sulfonyl in Drug Design".CHINESE JOURNAL OF ORGANIC CHEMISTRY 36.3(2016):490-501. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。