36026-83-2Relevant academic research and scientific papers
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.]
Synthesis and antiplatelet activity of phenyl quinolones
Huang, Li-Jiau,Hsieh, Ming-Chieh,Teng, Che-Ming,Lee, Kuo-Hsiung,Kuo, Sheng-Chu
, p. 1657 - 1662 (2007/10/03)
In our search for novel antiplatelet agents, seven positional phenyl quinolone isomers were synthesized. Preliminary screening confirmed their inhibitory effects against arachidonic acid (AA)-induced platelet aggregation. Varying the substitutional position of the phenyl group had a profound effect on the antiplatelet activity of these isomers. 3-Phenyl-4-quinolone showed the greatest potency and was superior to indomethacin, although the two structures are quite different. The mechanism and pharmacological action of 3-phenyl-4-quinolone are currently under investigation. Copyright (C) 1998 Elsevier Science Ltd.
