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Design and synthesis of novel conformationally restricted HIV protease inhibitors |
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| Authors: | Francesco G. Salituro Christopher T. Baker John J. Court David D. Deininger Eunice E. Kim Biquin Li Perry M. Novak Bhisetti G. Rao S. Pazhanisamy Margaret D. Porter Wayne C. Schairer Roger D. Tung |
| Affiliation: | Vertex Pharmaceuticals Incorporated, 130 Waverly Street, Cambridge, MA 02139, U.S.A. |
| 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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