Recommanded Product: 117918-23-7. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: (R)-3-(tert-Butoxycarbonyl)-5,5-dimethylthiazolidine-4-carboxylic acid, is researched, Molecular C11H19NO4S, CAS is 117918-23-7, about Small dipeptide-based HIV protease inhibitors containing the hydroxymethylcarbonyl isostere as an ideal transition-state mimic.
The human immunodeficiency virus (HIV) codes for an aspartic protease is known to be essential for retroviral maturation and replication. HIV protease is formed from two identical 99 amino acid peptides. Using the thioether chem. ligation method, [(NHCH2CH2-S-CH2CO)51-52, Ala67,95]HIV-1 protease was synthesized and then the [(NHCH2CH2-S-CH2CO)51-52, Ala67,95, Cys98]HIV-1 protease dimer analog covalently linked by a disulfide bridge was prepared These HIV-1 protease analogs effectively cleaved the Tyr-Phe-type substrate, but had weak affinity to the Tyr-Pro-type substrate. Consequently, the mol. recognition of the protease analogs differs from that of the wild-type enzyme. Based on the substrate transition state, a novel class of HIV protease inhibitors containing an unnatural amino acid, (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid, named allophenylnorstatine, with a hydroxymethylcarbonyl (HMC) isostere were designed and synthesized. The stereochem. of the hydroxyl group was significant for the enzyme inhibition and the HMC group interacted excellently with the aspartic acid carboxyl groups of HIV protease active site in the essentially same hydrogen-bonding mode as the transition state. Small dipeptide-based HIV protease inhibitors containing the HMC isostere were studied as advantageous compounds Among them, a dipeptide-based HIV protease inhibitor, KNI-577, exhibited potent antiviral activities, low cytotoxicity, and good pharmacokinetic properties.
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Reference:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts