28620-12-4, Name is 6-Nitro-2-benzothiazolinone, molecular formula is C7H4N2O3S, belongs to thiazole compound, is a common compound. In a patnet, once mentioned the new application about 28620-12-4, Recommanded Product: 28620-12-4
Elevated levels of active glucocorticoids have been implicated in the development of several phenotypes of metabolic syndrome, such as type2 diabetes and obesity. 11beta-Hydroxysteroid dehydrogenase type 1 (11beta-HSD1) catalyses the intracellular conversion of inactive cortisone to cortisol. Selective 11beta-HSD1 inhibitors have shown beneficial effects in various conditions, including diabetes, dyslipidemia and obesity. A series of adamantyl ethanone pyridyl derivatives has been identified, providing potent and selective inhibitors of human 11beta-HSD1. Lead compounds display low nanomolar inhibition against human and mouse 11beta-HSD1 and are selective for this isoform, with no activity against 11beta-HSD2 and 17beta-HSD1. Structure-activity relationship studies reveal that an unsubstituted pyridine tethered to an adamantyl ethanone motif through an ether or sulfoxide linker provides a suitable pharmacophore for activity. The most potent inhibitors have IC50 values around 34-48nM against human 11beta-HSD1, display reasonable metabolic stability in human liver microsomes, and weak inhibition of key human CYP450 enzymes.
Elevated levels of active glucocorticoids have been implicated in the development of several phenotypes of metabolic syndrome, such as type2 diabetes and obesity. 11beta-Hydroxysteroid dehydrogenase type 1 (11beta-HSD1) catalyses the intracellular conversion of inactive cortisone to cortisol. Selective 11beta-HSD1 inhibitors have shown beneficial effects in various conditions, including diabetes, dyslipidemia and obesity. A series of adamantyl ethanone pyridyl derivatives has been identified, providing potent and selective inhibitors of human 11beta-HSD1. Lead compounds display low nanomolar inhibition against human and mouse 11beta-HSD1 and are selective for this isoform, with no activity against 11beta-HSD2 and 17beta-HSD1. Structure-activity relationship studies reveal that an unsubstituted pyridine tethered to an adamantyl ethanone motif through an ether or sulfoxide linker provides a suitable pharmacophore for activity. The most potent inhibitors have IC50 values around 34-48nM against human 11beta-HSD1, display reasonable metabolic stability in human liver microsomes, and weak inhibition of key human CYP450 enzymes.
Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Recommanded Product: 28620-12-4. In my other articles, you can also check out more blogs about 28620-12-4
Reference£º
Thiazole | C3H7319NS – PubChem,
Thiazole | chemical compound | Britannica