| 摘要 |
The present invention includes a group of novel compounds that are demonstrated to potently and selectively inhibit HIV integrase (IN) activity in vitro and to potently inhibit HIV replication in live, cultured cells at non-toxic concentrations. The novel compounds disclosed include 2,3 -di(3,4- dihydroxydihydroxydihydrocinnamoyl) -L-tartaric acid, 2,3 -di-(3,4-dihydroxybenzoyl) -L-tartaric acid, 2,3 -di-(3,4 -dihydroxyphenylacetyl) -L-tartaric acid , 2,3 -di-(3,4,5 -trihydroxybenzoyl -L-tartaric acid, 2,3-dicaffeoyldiamidopropionic acid, 1,2,-dicaffeoyl -L-glyceric acid, bis, -3,4 -dicaffeoyldiamidobenzoic acid, di-3,4 -dihydroxybenzylidene succinic acid, di-3,4 -dihydrodihydroxybenzylidine succinic acid, 2,3 -dicaffeoyl-L-serine, bis-dicaffeoyl -L-isoserine and 1,4-dicaffeoyl -L-lysine. Tests of integrase inhibitors with 2',3'-dideoxycytidine, zidovudine and nelfinavir (protease inhibitor) indicated a potent synergy against reverse transcriptase inhibitor resistant virus. The potential benefit from the addition of integrase inhibitors to combination drug therapies is significant. |
