Synthesis of Zidovudine Derivatives with Anti-HIV-1 and Antibacterial Activities

CORC > 昆明动物研究所 > 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 > 分子免疫药理学

	Synthesis of Zidovudine Derivatives with Anti-HIV-1 and Antibacterial Activities
	Senthilkumar P 1; Long J 2; Swetha R 1; Shruthi V 1; Wang RR 2; Preethi S 1; Yogeeswari P 1; Zheng YT[]2; Sriram D[]1
刊名	NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
	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
内容类型	期刊论文
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.