19146-73-7Relevant articles and documents
Substituent-controlled chemoselective synthesis of multi-substituted pyridones: Via a one-pot three-component cascade reaction
Liu, Shitao,Li, Jisen,Lin, Junjie,Liu, Fujun,Liu, Teng,Huang, Chao
, p. 1130 - 1134 (2020)
An efficient and concise one-pot strategy for the synthesis of multisubstituted pyridones via a one-pot three-component cascade reaction catalyzed by Cs2CO3 under solvent-free conditions has been developed. The substituent-controlled chemoselective cycloaddition process involved steps including a Michael addition/ethanol elimination/intermolecular cyclization sequence utilizing anilines, diethyl acetylenedicarboxylate, and diethyl ethoxymethylenemalonate. In doing so, various 2-pyridone and 4-pyridone species (41 examples) could be obtained in good to excellent yields.
Novel quinolone-3-carboxylic acid derivatives as anti-HIV-1 agents: design, synthesis, and biological activities
Hajimahdi,Zabihollahi,Aghasadeghi,Ashtiani, S. Hosseini,Zarghi
, p. 1861 - 1876 (2016/10/03)
A new series of quinolone-3-carboxylic acids featuring different hydrophobic groups at N-1, C-2, C-7, and C-8 positions were synthesized and evaluated for their activity against single-cycle replicable HIV NL4-3 as inhibition rate of p24 expression in Hela cells cultures. Most of the synthesized compounds showed anti-HIV activity with no significant cytotoxicity at concentration of 100 μM. The most active compounds 4h, 4k, and 4j exhibited anti-HIV activity with an inhibition rate of 55, 71, and 84 %, respectively. A docking study using the crystallographic data available for PFV integrase including its complexes with Mg2+ and Raltegravir revealed that the active compounds could occupy same space near Raltegravir and interact with the Mg2+ ions in the active site. Thus, the anti-HIV activity of the synthesized compounds might involve a metal chelating mechanism. [InlineMediaObject not available: see fulltext.]
Design, synthesis, and biological evaluation of novel quinoline derivatives as HIV-1 Tat-TAR interaction inhibitors
Chen, Shuguang,Chen, Ran,He, Meizi,Pang, Ruifang,Tan, Zhiwu,Yang, Ming
experimental part, p. 1948 - 1956 (2009/05/26)
Thirty-two quinoline derivatives were designed and synthesized as HIV-1 Tat-TAR interaction inhibitors. All the compounds showed high antiviral activities in inhibiting the formation of SIV-induced syncytium in CEM174 cells. Nine of them with low cytotoxicities were evaluated by Tat dependent HIV-1 LTR-driven CAT gene expression colorimetric enzyme assay in human 293T cells, indicating effective inhibitory activities of blocking the Tat-TAR interaction. Molecular modeling experiments indicated that these compounds may inhibit Tat-TAR interaction by binding to Tat protein instead of TAR RNA.
