Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 117918-23-7, is researched, Molecular C11H19NO4S, about KNI-577, a potent small-sized HIV protease inhibitor based on the dipeptide containing the hydroxymethylcarbonyl isostere as an ideal transition-state mimic, the main research direction is HIV protease inhibitor KNI577 allophenylnorstatine isostere; KNI577 synthesis transition state structure antiviral.Quality Control of (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid.
Potent small-sized HIV protease inhibitors containing the hydroxymethylcarbonyl isostere were reported. The inhibitor KNI-727 with a dimethylmethoxyacetyl group in P2 position had a HIV protease inhibition of 95.9% at 50 nM and an anti-HIV activity EC50 of 1.73 μM in MT4 cells. Cyclization of the P2 moiety in KNI-549 resulted in the inhibitor KNI-577 (87.6% inhibition at 50 nM) with a remarkable anti-HIV-1(IIIB) activity (EC50=0.02 μM in CEM-SS cells). This antiviral activity was higher than that of the tripeptide KNI-272. KNI-577 had very low cytotoxicity (CC50>200 μM) and the bioavailability after intraduodenal administration in rats was 48%. A convenient synthetic scheme of KNI-577 was given.
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Reference:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts