1383786-08-0Relevant academic research and scientific papers
4-Substituted 2-hydroxyisoquinoline-1,3(2 H,4 H)-diones as a novel class of HIV-1 integrase inhibitors
Billamboz, Muriel,Suchaud, Virginie,Bailly, Fabrice,Lion, Cedric,Demeulemeester, Jonas,Calmels, Christina,Andreola, Marie-Line,Christ, Frauke,Debyser, Zeger,Cotelle, Philippe
supporting information, p. 606 - 611 (2013/07/26)
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.
