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Coordination of Histamine H3 Receptor Antagonists with Human Adrenal Cytochrome P450 Enzymes
Findings indicate direct coordination of these imidazole-containing H3 receptor antagonists with the heme moiety of human adrenal cytochrome P450 isozymes.
Pharmacological Characterization of the Novel Histamine H3-Receptor Antagonist N-(3,5-Dichlorophenyl)-N′-[[4-(1H-imidazol-4-ylmethyl)phenyl]-methyl]-urea (SCH 79687)
SCH 79687 is an orally active H3 antagonist with a good pharmacokinetic profile that, in combination with an H1 antagonist, demonstrates decongestant efficacy comparable with oral sympathomimetic decongESTants but without hypertensive liabilities.
Discovery of a Potent Pyrazolopyridine Series of γ-Secretase Modulators.
The synthesis and structure-activity relationship of a novel series of pyrazolopyridines represent a new class of γ-secretase modulators that demonstrate good in vitro potency in inhibiting Aβ42 production.
Development of novel benzomorpholine class of diacylglycerol acyltransferase I inhibitors.
The rational design of a novel class of DGAT1 inhibitors featuring a benzomorpholine core (23n) is reported, which conferred weight loss and a reduction in liver triglycerides when dosed chronically in mice with diet-induced obesity and depleted serum triglycerides following a lipid challenge.
Sch 50971, an orally active histamine H3 receptor agonist, inhibits central neurogenic vascular inflammation and produces sedation in the guinea pig.
Sch 50971 is an orally active, potent and selective agonist of Histamine H3 receptors that may act to ameliorate the sequelae of migraine headaches, where activation of histamine H2 receptors may be beneficial.
Discovery of a Novel Class of Orally Active Antifungal β-1,3-d-Glucan Synthase Inhibitors
A screen for antifungal bioactivities combined with mechanism-of-action studies identified a class of piperazinyl-pyridazinone compounds that target β-1,3-glucan synthase that exhibited in vitro activity comparable, and in some cases superior, to the echinocandins.
The discovery of fused oxadiazepines as gamma secretase modulators for treatment of Alzheimer's disease.
A novel pyrrolidine analog of histamine as a potent, highly selective histamine H3 receptor agonist.
Employing classical conformational analysis on a known H3 agonist, (R)-alpha-methylhistamine (1), a series of conformationally constrained H3 agonists were proposed and synthesized. Pyrrolidine
Pharmacology of a potent and selective inhibitor of PDE4 for inhaled administration.