BILLAMBOZ, Muriel; SUCHAUD, Virginie; BAILLY, Fabrice; LION, Cedric; DEMEULEMEESTER, Jonas; CALMELS, Christina; ANDRÉOLA, Marie-Line; CHRIST, Frauke; DEBYSER, Zeger; COTELLE, Philippe

doi:10.1021/ml400009t

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Article de revue

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ACS Medicinal Chemistry Letters. 2013-07-11, vol. 4, n° 7, p. 606-11

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A series of 2-hydroxy-1,3-dioxoisoquinoline-4-carboxamides featuring an N-hydroxyimide chelating functionality was evaluated for their inhibitory properties against human immunodeficiency virus type 1 integrase (HIV-1 IN). Several derivatives displayed low nanomolar IC50 values comparable to that of the clinically used raltegravir. A marked effect of one compound on both primary IN-catalyzed reactions, strand transfer (ST), and 3' processing (3'-P), emphasizes a novel IN inhibition mechanism establishing it as a potential new generation IN inhibitor. Substitution of the 2-hydroxyisoquinoline-1,3-dione scaffold at position 4 by carboxamido chains was beneficial for antiviral activity since reproducible low micromolar anti-HIV activities were obtained for the first time within this scaffold.< Leer menos

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2-hydroxy-1

3-dioxoisoquinoline-4-carboxamide; 3′ processing; HIV; antiretroviral; integrase

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https://oskar-bordeaux.fr/handle/20.500.12278/188691

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http://dx.doi.org/10.1021/ml400009t

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MFP (Laboratoire Microbiologie Fondamentale et Pathogénicité) - UMR 5234

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4-Substituted 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as a Novel Class of HIV-1 Integrase Inhibitors.

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