Investigation of a Novel Series of 2-Hydroxyisoquinoline-1, 3 (2 H, 4 H)-diones as Human Immunodeficiency Virus Type 1 Integrase Inhibitors

V Suchaud, F Bailly, C Lion, C Calmels…

Index: Suchaud, Virginie; Bailly, Fabrice; Lion, Cedric; Calmels, Christina; Andreola, Marie-Line; Christ, Frauke; Debyser, Zeger; Cotelle, Philippe Journal of Medicinal Chemistry, 2014 , vol. 57, # 11 p. 4640 - 4660

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Citation Number: 12

Abstract

We report herein further insight into the biological activities displayed by a series of 2- hydroxyisoquinoline-1, 3 (2 H, 4 H)-diones (HIDs). Substitution of the N-hydroxyimide two- metal binding pharmacophore at position 4 by carboxamido side chains was previously shown by us to be fruitful for this scaffold, since strong human immunodeficiency virus type 1 integrase (HIV-1 IN) inhibitors in the low nanomolar range associated with low micromolar ...