Suchaud, Virginie; Bailly, Fabrice; Lion, Cedric; Calmels, Christina; Andreola, Marie-Line; Christ, Frauke; Debyser, Zeger; Cotelle, Philippe published the artcile< Investigation of a Novel Series of 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as Human Immunodeficiency Virus Type 1 Integrase Inhibitors>, Application In Synthesis of 16426-64-5, the main research area is hydroxyisoquinolinedione preparation inhibition HIV1 integrase; structure hydroxyisoquinolinedione inhibition HIV1 integrase RNase H toxicity; mol docking hydroxyisoquinolinedione HIV1 integrase; physicochem property toxicity inhibition hERG CYP isoform hydroxyisoquinolinedione.
Hydroxyisoquinolinediones such as I (R = MeO, O2N, H2N, F, Cl, Br, F3C, NC, AcNH, PhCONH, 2-pyridinecarbonylamino, PhCH2CONH, 2-thiophenecarbonylamino; R1 = 4-FC6H4CH2, BuCH2CH2, Ph, PhCH2, 4-FC6H4, 4-FC6H4CH2CH2, 4-MeOC6H4CH2) (or their enol forms) were prepared as inhibitors of HIV-1 integrase; their inhibition of HIV-1 integrase, their anti-HIV-1 activities in human cells, their toxicities to human cells, and their inhibitions of RNase H were determined Introduction of electron-withdrawing functional groups such as a nitro moiety at position 7 of the isoquinoline ring led to a noticeable improvement in the antiviral activity of the resultant hydroxyisoquinolinediones with improved therapeutic indexes approaching those of the clin. used raltegravir while retaining potency against a panel of HIV-1 integrase mutants. The solubility, biol. permeability, transport by P-glycoprotein, inhibition of hERG and CYP isoforms, and specific cell toxicity effects of I (R = O2N; R1 = 4-FC6H4CH2) were determined
Journal of Medicinal Chemistry published new progress about Anti-HIV agents. 16426-64-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrNO4, Application In Synthesis of 16426-64-5.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary