HIV/AIDS

Novel integrase inhibitors highly active against HIV-1 in vitro

Published in AIDS Weekly, May 24th, 2004

Novel integrase inhibitors are highly active against HIV-1 in vitro.

"A series of 6-aryl-2,4-dioxo-5-hexenoic acids were synthesized and tested against HIV-1 in cell-based assays and against recombinant HIV-1 integrase (rIN) in enzyme assays," wrote investigators in Italy.

"Compound 8a showed potent antiretroviral activity (EC₅₀ = 1.5 mcM) and significant inhibition against ran (strand transfer: IC₅₀ = 7.9 mcM; 3'-processing: IC₅₀ = 7.0 mcM)," R. Costi and colleagues reported.

"A preliminary molecular modeling study was carried out to compare the spatial conformation of 8a with those of...

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Source: AIDS Weekly (2004-05-24)

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