New Developments in Diketo-Containing Inhibitors of HIV-1 Integrase

Author(s): Guisen Zhao, Chao Wang, Chuan Liu, Hongxiang Lou, Guisen Zhao, Chao Wang, Chuan Liu, Hongxiang Lou.

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 7 , Issue 7 , 2007


HIV-1 integrase is one of the three enzymes, which are critical for viral replication. It catalyzes the integration of the HIV genome into the cellular chromosome. Since there is no known human homolog to integrase, its inhibition is one of the most promising novel drug targets for anti-retroviral therapy with potential advantage over existing therapies. To date, numerous compounds with diverse structural features have been reported as integrase inhibitors, among which the diketo-containing inhibitors of HIV-1 integrase represent a major lead for anti-HIV drug development. The discovery of diketo acids plays an important role in validating integrase as a legitimate target for treatment of AIDS. In this review, we summarize several drug candidates in clinical trials and new diketo-containing inhibitors of HIV-1 integrase discovered recently.

Keywords: Human immunodeficiency virus, integrase, inhibitors, diketo acids

Rights & PermissionsPrintExport

Article Details

Year: 2007
Page: [707 - 725]
Pages: 19
DOI: 10.2174/138955707781024535
Price: $58

Article Metrics

PDF: 7
PRC: 0