Design, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1, 3 (2 H, 4 H)-diones as dual inhibitors of human immunodeficiency virus type 1 …

…, M Witvrouw, F Christ, Z Debyser…

Index: Barreca, Maria Letizia; Ferro, Stefania; Rao, Angela; De Luca, Laura; Zappala, Maria; Monforte, Anna-Maria; Debyser, Zeger; Witvrouw, Myriam; Chimirri, Alba Journal of Medicinal Chemistry, 2005 , vol. 48, # 22 p. 7084 - 7088

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Citation Number: 82

Abstract

We report herein the synthesis of a series of 19 2-hydroxyisoquinoline-1, 3 (2 H, 4 H)-dione derivatives variously substituted at position 7 aimed at inhibiting selectively two-metal ion catalytic active sites. The compounds were tested against HIV-1 reverse transcriptase (RT) polymerase, HIV-1 RT ribonuclease H (RNase H), and HIV-1 integrase (IN). Most compounds displayed poor inhibition of RT polymerase even at 50 μM. The majority of the ...

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