| 摘要 |
FIELD: organic chemistry. SUBSTANCE: invention relates to novel chemical compound, namely, to glycyrrhizic acid amide with 5-aminouracil of the formula (I) where R means OH (Ia) or R means (Ib) eliciting anti-HIV-activity in cultured cells MT-4. This compound inhibits accumulation of virus-specific protein p24 with high efficiency (ID50 = 55 mcg/ml, or 52.8 mcM), total viral antigen (ID50 = 75 mcg/ml, or 72.0 mcM) that reduces activity of reverse transcriptase (revertase; RT) (ID50 = 55 mcg/ml, or 52.8 mcM). Chemotherapeutic index (IS) of this compound is 27.7-277.3 by different parameters that exceeds that for glycyrrhizic acid significantly (4.4-24.0) and provides effective protection of cells MT-4 from the death (102-123%) as result of HIV-infection. Protective effect of this compound exceeds the protective effect of glycyrrhizic acid and azidothymidine and, in contrast to the latter, toxicity of glycyrrhizic acid amide with 5-aminouracil by about 540-fold less for cells (ID50 = 2080 mcg/ml, or 1998 mcM). EFFECT: improved pharmacological properties of compound. 2 cl, 2 tbl, 2 ex |
