Amide-containing diketoacids as HIV-1 integrase inhibitors: Synthesis, structure–activity relationship analysis, and biological activity
摘要:
HIV-1 integrase, which catalyzes the integration of the viral genome into the cellular chromosome, is an essential enzyme for retroviral replication, and represents an attractive and validated target in the development of therapeutics against AIDS. In this paper, 17 amide-containing novel diketoacids were designed and synthesized, and their ability to inhibit HIV-1 integrase was tested. The structure-activity relationships were also analyzed. (C) 2009 Elsevier Ltd. All rights reserved.
HIV-1 integrase, which catalyzes the integration of the viral genome into the cellular chromosome, is an essential enzyme for retroviral replication, and represents an attractive and validated target in the development of therapeutics against AIDS. In this paper, 17 amide-containing novel diketoacids were designed and synthesized, and their ability to inhibit HIV-1 integrase was tested. The structure-activity relationships were also analyzed. (C) 2009 Elsevier Ltd. All rights reserved.
efficient, reusable and stable binaphthyl stabilized Pd‐nanoparticles (Pd‐BNP) catalyzed the direct ortho‐C−H hydroxylation of acetophenone oxime ethers under neutral and phosphineligand‐free condition has been developed. A readily available, economic, safe and greener oxidant oxone has been used in this direct ortho‐hydroxylation. The scope of the reaction has been studied with various acetophenone oxime