364753-22-0Relevant academic research and scientific papers
Dicaffeoyl- or digalloyl pyrrolidine and furan derivatives as HIV integrase inhibitors
Hwang, Dong Jin,Kim, Sun Nam,Choi, Jung Hoon,Lee, Yong Sup
, p. 1429 - 1437 (2007/10/03)
Human immunodeficiency virus (HIV) integrase (IN) catalyzes the integration of HIV DNA copy into the host cell DNA. Such integration is essential for the production of progeny viruses, and therefore therapeutic agents that can inhibit this process should be effective anti-HIV agents. We have previously reported the inhibitory activity of dicaffeoylglucoside against HIV IN. In the present study, we have synthesized and tested dicaffeoyl or digalloyl compounds joined through a five-membered heterocyclic ring as HIV IN inhibitors to explore the SARs of this family of compounds. The starting heterocyclic diols were prepared from L-tartaric acid, diethyl L-tartarate or D-(+)-ribonic γ-lactone. We found that the HIV IN inhibitory activities of dicaffeoyl derivatives were comparable to that of L-chicoric acid (IC50 = 24.9μM). On the other hand, digalloyl derivatives were more potent than L-chicoric acid with IC50 values of 4.7-15.6μM. Copyright
