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  • Title: Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors.
    Author: Baker CT, Salituro FG, Court JJ, Deininger DD, Kim EE, Li B, Novak PM, Rao BG, Pazhanisamy S, Schairer WC, Tung RD.
    Journal: Bioorg Med Chem Lett; 1998 Dec 15; 8(24):3631-6. PubMed ID: 9934484.
    Abstract:
    A combination of structure-based design and both solution, and solid-phase synthesis were utilized to derive a potent (nM) series of HIV-1 protease inhibitors bearing a structurally novel backbone. Detailed structural analysis of several inhibitors prepared in this series has suggested that rigidification of the P1/P2 region of this class of molecules may result in compounds with improved potency.
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