359780-60-2Relevant academic research and scientific papers
Lysine derivatives as potent HIV protease inhibitors. Discovery, synthesis and structure-activity relationship studies
Bouzide, Abderrahim,Sauve, Gilles,Yelle, Jocelyn
, p. 1509 - 1513 (2007/10/03)
A screening assay program on HIV-protease was carried out on more than fifty commercially available N-protected amino acids and has revealed that those with a long side chain such as lysine, ornithine and arginine exhibited significant inhibition of HIV protease enzyme. The presence of an Fmoc group was found to be essential to obtain micromolar inhibitors and the addition of an alkyl group at the Nα-position resulted in the discovery of the lead compound 11 displaying a 5 nM inhibition constant. Although this new inhibitor series is not categorized among those mimicking the substrate with a non-hydrolyzable transition-state isoster, it was found very specific to inhibit HIV protease enzyme in comparison to the mammalian aspartyl proteases pepsin, renin and cathepsin. Furthermore, these inhibitors did not show any cytotoxicity at a concentration below 75 μM.
Urea derivatives as HIV aspartyl protease inhibitors
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, (2008/06/13)
The present invention provides HIV aspartyl protease inhibitors of the formula: and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein n is 3 or 4, Y is O, S, NH or N—CN, wherein Cx may be,
HIV protease inhibitors based on amino acid derivatives
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, (2008/06/13)
A compound selected from the group consisting of a compound of formula I 1a compound of formula II 2and when the compound of formula I and II comprises an amino group pharmaceutically acceptable ammonium salts thereof, wherein R1, R2, Cx, n, R3, R4, R5, Y are as defined in the specification.
Amino acid derivatives as HIV aspartyl protease inhibitors
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, (2008/06/13)
The present invention relates to a class of amino acid derivatives with HIV aspartyl protease inhibitory properties.
