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The anti-HIV activity of three 2-alkylsulfanyl-6-benzyl-3, 4- dihydropyrimidin-4 (3H)-one derivatives acting as non-nucleoside reverse transcriptase inhibitor in vitro

文献类型：期刊论文

作者Long J1,3; Zhang DH2; Zhang GH1; Rao ZK2; Wang YH1; Tam SC4; He YP[*]2; Zheng YT[*]1
刊名药学学报
出版日期2010
卷号45期号:2页码:228-234
关键词AIDS HIV-1 reverse transcriptase NNRTIs S-DABOs anti-HIV activity
其他题名三个非核苷类逆转录酶抑制剂 S-DABO 类衍生物的体外抗 HIV 作用
通讯作者yphe@ynu.edu.cn ; zhengyt@mail.kiz.ac.cn
合作状况其它
中文摘要本文对3个新S-DABO类衍合物(RZK-4、RZK-5、RZK-6)的体外抗HIV活性进行了研究。化合物RZK-4、RZK-5和RZK-6在200μg·mL-1的浓度下均能完全抑制HIV-1逆转录酶的活性。3个化合物对多种细胞均呈现出低毒性,且均在较低浓度下具有抑制HIV-1病毒实验株、临床株和耐药株的作用,治疗指数为3704～38462。其中,化合物RZK-6对HIV-1耐药株HIV-1IIIBA17具有非常显著的抑制作用。结果表明,这3种S-DABO类衍生物有良好的体外抗HIV-1作用,具有开发成为抗HIV-1药物的前景。
英文摘要It was recently shown that several new synthetic 2-alkylsulfanyl-6-benzyl-3, 4-dihydropyrimidin- 4(3H)-one (S-DABO) derivatives demonstrated anti-HIV-1 activity. Three of the derivatives namely RZK-4, RZK-5 and RZK-6 were used in this study to explore their inhibitory effects on a variety of HIV strains. These compounds at a concentration of 200 µg·mL −1 almost completely inhibited the activity of recombinant HIV-1 reverse transcriptase. All of the three compounds reduced replication of HIV-1 laboratory-derived strains, low-passage clinical isolated strain, and the drug resistant strain. In particular RZK-6 showed potent activity against the HIV-1 drug resistant strain. In general, the antiviral activities are similar in magnitude to nevirapine (NVP), which is a non-nucleoside reverse transcriptase inhibitor approved by FDA. The therapeutic indexes of these compounds were remarkable, ranging from 3 704 to 38 462 indicating extremely low cytotoxicity. These results suggest that the three S-DABO derivatives in this study have good potential for further development in anti-HIV-1 therapy. It may be particularly useful to target at the non-nucleoside reverse transcriptase inhibitors resistant HIV-1 strain.
收录类别其他
资助信息Project supported in part by grants from NSFC (39970851, 30560179); 863 Program (2006AA020602); 973 Program (2009CB522306); Key Scientific and Technology Projects of China (2008ZX10001-015, 2009ZX09501-029); and Yunnan (2007BC006, 2009BC018), CAS (KSCX1-YW-R-24).
语种英语
公开日期2010-08-19
源URL[http://159.226.149.42:8088/handle/152453/1730]  
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.Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223
2.Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China
3.Graduate School of Chinese Academy of Sciences, Beijing 100039, China
4.Department of Physiology, Chinese University of Hong Kong, Hong Kong SAR, China
推荐引用方式
GB/T 7714		 Long J,Zhang DH,Zhang GH,et al. The anti-HIV activity of three 2-alkylsulfanyl-6-benzyl-3, 4- dihydropyrimidin-4 (3H)-one derivatives acting as non-nucleoside reverse transcriptase inhibitor in vitro[J]. 药学学报,2010,45(2):228-234.
APA Long J.,Zhang DH.,Zhang GH.,Rao ZK.,Wang YH.,...&Zheng YT[*].(2010).The anti-HIV activity of three 2-alkylsulfanyl-6-benzyl-3, 4- dihydropyrimidin-4 (3H)-one derivatives acting as non-nucleoside reverse transcriptase inhibitor in vitro.药学学报,45(2),228-234.
MLA Long J,et al."The anti-HIV activity of three 2-alkylsulfanyl-6-benzyl-3, 4- dihydropyrimidin-4 (3H)-one derivatives acting as non-nucleoside reverse transcriptase inhibitor in vitro".药学学报 45.2(2010):228-234.

入库方式： OAI收割

来源：昆明动物研究所

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