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-dihydroxy-dihydroxydihydrocinnamoyl)-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.