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