| Literature DB >> 9871528 |
J D Rodgers1, B L Johnson, H Wang, S Erickson-Viitanen, R M Klabe, L Bacheler, B C Cordova, C H Chang.
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.Entities:
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Year: 1998 PMID： 9871528 DOI： 10.1016/s0960-894x(98)00118-8
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823