Design and synthesis of novel conformationally restricted HIV protease inhibitors |
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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 |
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Affiliation: | Vertex Pharmaceuticals Incorporated, Cambridge, MA 02139, USA. |
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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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