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6-Benzoxazinylpyridazin-3-ones: potent, long-acting positive inotrope and peripheral vasodilator agents.
Positive inotropic activity was maintained for between 8 and 24 h after a single oral dose of bemoradan in dogs, thus making it one of the most potent and long-acting orally effective inotropes yet described.
Benzoxazinones as PPARgamma agonists. 2. SAR of the amide substituent and in vivo results in a type 2 diabetes model.
In vivo analysis with 13 and 57 demonstrated that the series of benzoxazinones synthesized and tested for PPARgamma agonist activity has potential for the treatment of type 2 diabetes.
Discovery of selective imidazole-based inhibitors of mammalian 15-lipoxygenase: highly potent against human enzyme within a cellular environment.
Design, synthesis and bronchodilatory activity of a series of quinazoline-3-oxides.
A synthetic program of rational drug design was undertaken to develop a series of quinazoline-3-oxides as pulmonary-selective inhibitors of ovalbumin-induced, leukotriene-mediated bronchoconstriction, with significant enhancement in selectivity.
Substituted quinazoline 3 oxides providing pharmacological activity us patent 4745118. may 17 1988
Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase.
Pyrazole-based sulfonamide and sulfamides as potent inhibitors of mammalian 15-lipoxygenase.
Nonsteroidal progesterone receptor ligands. 1. 3-Aryl-1-benzoyl-1,4,5,6-tetrahydropyridazines.
Nonsteroidal progesterone receptor ligands. 2. High-affinity ligands with selectivity for bone cell progesterone receptors.
A novel series of nonsteroidal heterocycles was discovered which display cell-type selective, high-affinity (nanomolar) binding to the progesterone receptors from TE85 osteosarcoma cells but > 1…