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-dihydropyrimidin4（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.