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Design and synthesis of novel conformationally restricted HIV protease inhibitors
Authors:FG Salituro  CT Baker  JJ Court  DD Deininger  EE Kim  B Li  PM Novak  BG Rao  S Pazhanisamy  MD Porter  WC Schairer  RD Tung
Affiliation:Vertex Pharmaceuticals Incorporated, Cambridge, MA 02139, USA.
Abstract:A set of HIV protease inhibitors represented by compound 2 has previously been described. Structural and conformational analysis of this compound suggested that conformational restriction of the P1/P2 portion of the molecule could lead to a novel set of potent protease inhibitors. Thus, probe compounds 3-7 were designed, synthesized, and found to be potent inhibitors of HIV protease.
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