Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors |
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Authors: | CT Baker FG Salituro JJ Court DD Deininger EE Kim B Li PM Novak BG Rao S Pazhanisamy WC Schairer RD Tung |
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Affiliation: | Vertex Pharmaceuticals Incorporated, Cambridge, MA 02139, USA. |
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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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