title: [Advances in the study of HIV-1 integrase inhibitors of alpha, gamma-diketo compounds].
abstract: HIV-1 integrase (IN) is an essential enzyme for retroviral replication. There is no analogue for this enzyme in human cells so that inhibition of IN will not bring strong effect on human body. Thus, HIV-1 IN has become a rational target for therapy of AIDS. This review provides a comprehensive report of alpha, gamma-diketo IN inhibitors discovered in recent years. Compilation of such data will prove to be beneficial in developing QSAR, pharmacophore hypothesis generation and validation, virtual screening and synthesis of compounds with higher activity.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Jinan 250012, China.
authors.forename: Sheng-hui
authors.initials: SH
authors.lastname: Yu
authors.forename: Yan-mei
authors.initials: YM
authors.lastname: Tan
authors.forename: Gui-sen
authors.initials: GS
authors.lastname: Zhao
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D019427:HIV Integrase / Q000737:chemistry / Q000502:physiology; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D007651:Keto Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D021281:Quantitative Structure-Activity Relationship
chemical_list: D019380:Anti-HIV Agents; D019428:HIV Integrase Inhibitors; D007651:Keto Acids; D019427:HIV Integrase