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Paper | Regular issue | Vol 78, No. 4, 2009, pp.947-959
Published online, 5th December, 2008
DOI: 10.3987/COM-08-11573
Structural Modification of Diketo Acid Portion in 1H-Benzylindole Derivatives HIV-1 Integrase Inhibitors

Stefania Ferro,* Sara De Grazia, Laura De Luca, Maria Letizia Barreca, Zeger Debyser, and Alba Chimirri

*Department of Medicinal Chemistry, University of Messina, Viale Annunziata, 98168 Messina, Italy

Abstract

Our previous studies led to discovery of a very potent benzylindoldiketo acid (CHI-1043) acting as HIV-1 integrase strand transfer inhibitor. We herein report the synthesis of new structurally different compounds in which the 1,3-diketo acid moiety has been substituted with other functionalities. The synthesized derivatives were evaluated for their activity on the IN enzyme and in MT-4 cells but only 4-[1-(4-fluorobenzyl)-4-methoxy-1H-indol-3-yl)-3-hydroxyfuran-2(5H)-one (12) was able to strongly inhibit HIV-1 probably by biotransformation into CHI-1043.