2007

Indole derivativesR 0140 New 4-[(1-Benzyl-1H-indol-3-yl)carbonyl]-3-hydroxyfuran-2(5H)-ones, β-Diketo

Acid Analogues as HIV-1 Integrase Inhibitors. — Design, synthesis and biological activity of a series of furan derivatives (IV) (10 examples) and related β-diketo acids (V) are described. Derivative (IVb) proves to be an interesting integrase inhibitor. How-ever, even if the furanone derivatives generally exhibit good potency in the micromolar range, they diminish potency both in enzymatic and cell assays with a low selectivity profile compared to the corresponding diketo acids and esters. — (FERRO*, S.; BARRECA, M. L.; DE LUCA, L.; RAO, A.; MONFORTE, A. M.; DEBYSER, Z.; WITVROUW, M.; CHIMIRRI, A.; Arch. Pharm. (Weinheim, Ger.) 340 (2007) 6, 292-298; Dip. Farm.-Chim., Univ. Messina, I-98168 Messina, Italy; Eng.) — A. Forchert

41- 098