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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。
In this paper, three novel S-DABO derivatives (RZK-4, RZK-5, RZK-6) were studied in vitro for their anti-HIV activity. Compounds RZK-4, RZK-5 and RZK-6 completely inhibited the activity of HIV-1 reverse transcriptase at a concentration of 200 μg · mL-1. The three compounds showed low toxicity to a variety of cells, and all of them inhibited the HIV-1 virus experimental strains, clinical strains and drug-resistant strains at a lower concentration, and the therapeutic index was 3704-38462. Among them, the compound RZK-6 has a very significant inhibitory effect on the HIV-1 drug-resistant strain HIV-1IIIBA17. The results show that these three derivatives of S-DABO have a good anti-HIV-1 effect in vitro and have the prospect of being developed as anti-HIV-1 drugs.