1084815-99-5Relevant articles and documents
Discovery of 3-acetyl-4-hydroxy-2-pyranone derivatives and their difluoridoborate complexes as a novel class of HIV-1 integrase Inhibitors
Ramkumar, Kavya,Tambov, Konstantin V.,Gundla, Rambabu,Manaev, Alexandr V.,Yarovenko, Vladimir,Traven, Valery F.,Neamati, Nouri
, p. 8988 - 8998 (2008)
HIV-1 integrase (IN) has emerged as an important therapeutic target for anti-HIV drug development. Its uniqueness to the virus and its critical role in the viral life cycle makes IN suitable for selective inhibition. The recent approval of Raltegravir (MK-0518) has created a surge in interest and great optimism in the field. In our ongoing IN drug design research, we herein report the discovery of substituted analogs of 3-acetyl-4-hydroxy-2-pyranones and their difluoridoborate complexes as novel IN inhibitors. In many of these compounds, complexation with boron difluoride increased the potency and selectivity of IN inhibition. Compound 9 was most active with an IC50 value of 9 μM and 3 μM for 3'-processing and strand transfer inhibition, respectively.
Synthesis and reactions of dehydracetic acid difluoroborane complex
Manaev,Tambov,Traven'
experimental part, p. 1054 - 1060 (2009/07/05)
Dehydracetic acid difluoroborane complex, 3-acetyl-6-methyl-2-oxo-2H-pyran- 4-yl difluoridoborate, was synthesized and characterized. The complex was involved into condensation reactions at the acetyl group with various aromatic and heterocyclic aldehydes
