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  • Title: A new class of HIV-1 protease inhibitors containing a tertiary alcohol in the transition-state mimicking scaffold.
    Author: Ekegren JK, Unge T, Safa MZ, Wallberg H, Samuelsson B, Hallberg A.
    Journal: J Med Chem; 2005 Dec 15; 48(25):8098-102. PubMed ID: 16335934.
    Abstract:
    Novel HIV-1 protease inhibitors encompassing a tertiary alcohol as part of the transition-state mimicking unit have been synthesized. Variation of the P1'-P3' residues and alteration of the tertiary alcohol absolute stereochemistry afforded 10 inhibitors. High potencies for the compounds with (S)-configuration at the carbon carrying the tertiary hydroxyl group were achieved with Ki values down to 2.4 nM. X-ray crystallographic data for a representative compound in complex with HIV-1 protease are presented.
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