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Synthesis and antiviral activity of P1' arylsulfonamide azacyclic urea HIV protease inhibitors |
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| Authors: | Huang Peggy P Randolph John T Klein Larry L Vasavanonda Sudthida Dekhtyar Tatyana Stoll Vincent S Kempf Dale J |
| Institution: | Abbott Laboratories, Infectious Disease Research, Dept. R47D, Building AP52N, 200 Abbott Park Road, Abbott Park, IL 60064-6217, USA. peggy.huang@abbott.com |
| Abstract: | A series of novel azacyclic urea HIV protease inhibitors bearing a benzenesulfonamide group at P1' were synthesized utilizing a parallel synthesis method. Structural studies of early analogs bound in the enzyme active site were used to design more potent inhibitors. The effects of substituting the P1' benzenesulfonyl group on antiviral activity and protein binding are described. |
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