Synthesis and antiplatelet activity of phenyl quinolones

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...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry 1998-10, Vol.6 (10), p.1657-1662
Main Authors: Huang, L J, Hsieh, M C, Teng, C M, Lee, K H, Kuo, S C
Format: Article
Language:English
Subjects:
Animals
Isomerism
Platelet Aggregation Inhibitors - chemical synthesis
Platelet Aggregation Inhibitors - chemistry
Platelet Aggregation Inhibitors - pharmacology
Quinolones - chemical synthesis
Quinolones - chemistry
Quinolones - pharmacology
Rabbits
Structure-Activity Relationship
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:0968-0896
DOI:10.1016/s0968-0896(98)00141-2