Ontology highlight
ABSTRACT:
SUBMITTER: Billamboz M
PROVIDER: S-EPMC4027527 | biostudies-literature | 2013 Jul
REPOSITORIES: biostudies-literature
Billamboz Muriel M Suchaud Virginie V Bailly Fabrice F Lion Cedric C Demeulemeester Jonas J Calmels Christina C Andréola Marie-Line ML Christ Frauke F Debyser Zeger Z Cotelle Philippe P
ACS medicinal chemistry letters 20130517 7
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 est ...[more]