Synthesis and evaluation of (S,S)-N,N '-bis-[3-(2,2 ',6,6 '-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) analogs with anti-tuberculosis activity
文献类型：期刊论文
| 作者 | Zhang, Xuelian6; Hu, Yanwei4,5; Chen, Shudan6; Luo, Rusong6; Yue, Jun1; Zhang, Ying3; Duan, Wenhu2 ; Wang, Honghai6
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2009-11-01 |
| 卷号 | 19期号:21页码:6074-6077 |
| 关键词 | Antitubercular drug Resistance MIC |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2009.09.035 |
| 文献子类 | Article |
| 英文摘要 | In order to identify new and potent candidate drugs to treat tuberculosis, a library of compounds was screened, and (S,S)-N,N '-bis-[3-(2,2 ',6,6 '-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) was identified as a hit in the screen. This research discusses our efforts to synthesize and test 30 analogs of this hit for activity against Mycobacterium tuberculosis. Two compounds with homopiperazine ring possess high in vitro activity against drug sensitive and resistant M. tuberculosis with MICs 0.78-3.13 mu g/mL (or 1.22-4.88 mu M). (C) 2009 Elsevier Ltd. All rights reserved. |
| WOS关键词 | COMBINATORIAL LEAD OPTIMIZATION ; DRUG-RESISTANT TUBERCULOSIS ; IN-VITRO ; DERIVATIVES ; ETHAMBUTOL ; SQ109 ; VIVO ; TB |
| 资助项目 | 863 high-tech project[2007AA02Z316] ; national natural science foundation of China[30901828] ; Shanghai science and technology funding[06JC14012] ; severe infectious disease project[2008ZX10003-006-2] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000270561300018 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279090]  |
| 专题 | 药物化学研究室 |
| 通讯作者 | Wang, Honghai |
| 作者单位 | 1.Shanghai Pulm Hosp, Dept Clin Lab, Shanghai, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, Shanghai 200031, Peoples R China 3.Johns Hopkins Univ, Dept Mol Microbiol & Immunol, Bloomberg Sch Publ Hlth, Baltimore, MD USA; 4.Soochow Univ, Sch Pharm, Coll Med, Suzhou, Peoples R China; 5.Fudan Univ, Dept Med Chem, Shanghai 200433, Peoples R China; 6.Fudan Univ, Inst Genet, State Key Lab Genet Engn, Sch Life Sci, Shanghai 200433, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Zhang, Xuelian,Hu, Yanwei,Chen, Shudan,et al. Synthesis and evaluation of (S,S)-N,N '-bis-[3-(2,2 ',6,6 '-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) analogs with anti-tuberculosis activity[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2009,19(21):6074-6077. |
| APA | Zhang, Xuelian.,Hu, Yanwei.,Chen, Shudan.,Luo, Rusong.,Yue, Jun.,...&Wang, Honghai.(2009).Synthesis and evaluation of (S,S)-N,N '-bis-[3-(2,2 ',6,6 '-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) analogs with anti-tuberculosis activity.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,19(21),6074-6077. |
| MLA | Zhang, Xuelian,et al."Synthesis and evaluation of (S,S)-N,N '-bis-[3-(2,2 ',6,6 '-tetramethylbenzhydryloxy)-2-hydroxy-propyl]-ethylenediamine (S2824) analogs with anti-tuberculosis activity".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 19.21(2009):6074-6077. |
入库方式： OAI收割
来源：上海药物研究所
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