2-Hydroxyisoquinoline-1, 3 (2H, 4H)-diones as inhibitors of HIV-1 integrase and reverse transcriptase RNase H domain: influence of the alkylation of position 4

…, Z Debyser, L De Luca, A Chimirri, P Cotelle

Index: Billamboz, Muriel; Bailly, Fabrice; Lion, Cedric; Calmels, Christina; Andreola, Marie-Line; Witvrouw, Myriam; Christ, Frauke; Debyser, Zeger; De Luca, Laura; Chimirri, Alba; Cotelle, Philippe European Journal of Medicinal Chemistry, 2011 , vol. 46, # 2 p. 535 - 546

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Citation Number: 36

Abstract

We report herein the synthesis of a series of fifteen 2-hydroxyisoquinoline-1, 3 (2H, 4H)- dione derivatives. Alkyl and arylalkyl groups were introduced on position 4 of the basis scaffold. All the compounds presented poor inhibitory properties against HIV-1 reverse transcriptase ribonuclease H (RNase H). Four compounds inhibited HIV-1 integrase at a low micromolar level. A docking study using the later crystallographic data available for PFV ...