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  • Title: Potent cyclic urea HIV protease inhibitors with 3-aminoindazole P2/P2' groups.
    Author: Rodgers JD, Johnson BL, Wang H, Erickson-Viitanen S, Klabe RM, Bacheler L, Cordova BC, Chang CH.
    Journal: Bioorg Med Chem Lett; 1998 Apr 07; 8(7):715-20. PubMed ID: 9871528.
    Abstract:
    Cyclic ureas containing 3-aminoindazole P2/P2' groups are extremely potent inhibitors of HIV protease. The parent 3-aminoindazole 6 showed a Ki < 0.01 nM but poor translation of enzyme activity to antiviral activity was observed. A series of 3-alkylaminoindazoles revealed that translation improved with increasing lipophilicity. An X-ray crystal structure of 6 bound to HIV protease was obtained.
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