Synthesis of Zidovudine Derivatives with Anti-HIV-1 and Antibacterial Activities
文献类型：期刊论文
| 作者 | Senthilkumar P1; Long J2; Swetha R1; Shruthi V1; Wang RR2; Preethi S1; Yogeeswari P1; Zheng YT[*]2; Sriram D[*]1 |
| 刊名 | NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
 |
| 出版日期 | 2009 |
| 卷号 | 28期号:2页码:89-102 |
| ISSN号 | 1525-7770 |
| 通讯作者 | drdsriram@yahoo.com ; zhengyt@mail.kiz.ac.cn |
| 合作状况 | 其它 |
| 英文摘要 | Twelve novel zidovudine derivatives were prepared by modifying 5 '-hydroxyl group of sugar moiety (1-8) and 5-methyl group of thymidine nucleus (9-12) and characterized spectrally. The compounds were evaluated for anti-HIV-1, antitubercular and antibacterial activities. Compound (3-azido-tetrahydro-5- (3,4-dihydro-5-methyl-2,4-dioxopyrimidin- 1 (2H)-yl) furan-2-yl)methyl 7- (4- (2-phenylacetoyloxy) -3,5- dimethylpiperazin-1-yl) -5- (2-phenylacetoyloxyamino) -1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylate (5) was found to be the most potent anti-HIV-1 agent with EC50 of 0.0012 M against HIV-1IIIB and CC50 of 34.05 M against MT-4 with selectivity index of 28,375. Compound 5 inhibited Mycobacterium tuberculosis with MIC of 1.72 M and inhibited four pathogenic bacteria with MIC of less than 1 M. |
| 收录类别 | SCI |
| 资助信息 | This study was supported by grants from the CAS (KSCX1-YW-R-24), National 973 project of China (2006CB504200), Key Scientific and Technological projects of China (2004BA719A14), and Yunnan (2004NG12). |
| 原文出处 | 200928289.pdf |
| 语种 | 英语 |
| 公开日期 | 2010-08-24 |
| 源URL | [http://159.226.149.42:8088/handle/152453/4681]  |
| 专题 | 昆明动物研究所_分子免疫药理学 昆明动物研究所_动物模型与人类重大疾病机理重点实验室 |
| 作者单位 | 1.Medicinal Chemistry & Antimycobacterial Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science{Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad, Andhra Pradesh, India 2.Laboratory of Molecular Immunopharmacology, Key Laboratory of Animal Models and Human Diseases Mechanisms, Kunming Institute of Zoology, The Chinese Academy of Sciences, Kunming, Yunnan, P. R. China |
| 推荐引用方式 GB/T 7714 | Senthilkumar P,Long J,Swetha R,et al. Synthesis of Zidovudine Derivatives with Anti-HIV-1 and Antibacterial Activities[J]. NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS,2009,28(2):89-102. |
| APA | Senthilkumar P.,Long J.,Swetha R.,Shruthi V.,Wang RR.,...&Sriram D[*].(2009).Synthesis of Zidovudine Derivatives with Anti-HIV-1 and Antibacterial Activities.NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS,28(2),89-102. |
| MLA | Senthilkumar P,et al."Synthesis of Zidovudine Derivatives with Anti-HIV-1 and Antibacterial Activities".NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS 28.2(2009):89-102. |
入库方式： OAI收割
来源：昆明动物研究所
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