Based on the mode of action, the present paper reviews the HIV-1 integrase inhibitors reported recently with respect to the structure features, pharmacophore analysis, chemical synthesis and the development status, according to the categories of strand transfer inhibitor, IN-DNA interaction inhibitor, 3’-processing inhibitor, non-specific inhibitor and peptide inhibitor, respectively. The strand transfer inhibitor is the most developed class of HIV-1 integrase inhibitors, among which MK-0518 was the first FDA-approved HIV-1 integrase inhibitor as anti-HIV drug. HIV-1 integrase inhibitor has enriched the highly active antiretroviral therapy (HAART) regimen and provides an efficient treatment for multiple drug-resistant patients.

Key words: HIV-1 integrase, inhibitor, anti-HIV drug, GS-9137, raltegravir (MK-0518)