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Quantitative structure-activity relationships of 5-lipoxygenase inhibitors. Inhibitory potency of pyridazinone analogues.

Authors :
Kim KH
Martin YC
Brooks DW
Dyer RD
Carter GW
Source :
Journal of pharmaceutical sciences [J Pharm Sci] 1994 Mar; Vol. 83 (3), pp. 433-8.
Publication Year :
1994

Abstract

Quantitative structure-activity relationships (QSAR) of 72 1-phenyltetrahydropyridazin-3(2H)-one (I) analogues are examined for the inhibitory potency (IC50) of 5-lipoxygenase in a broken cell. The potency is increased by lipophilic substituents at the 3'- and 4'-positions. Substituents with positive F value at the 4'-position also increase the potency, while substituents at the 3'-position with a positive R value decrease it. The potency also decreases as the size of the 2'- and/or 4'-substituents increases. Thioketone analogues are about 5 times more potent than the corresponding carbonyl analogues.

Details

Language :
English
ISSN :
0022-3549
Volume :
83
Issue :
3
Database :
MEDLINE
Journal :
Journal of pharmaceutical sciences
Publication Type :
Academic Journal
Accession number :
8207697
Full Text :
https://doi.org/10.1002/jps.2600830334