Lachance, Nicolas published the artcileDiscovery of potent and liver-targeted stearoyl-CoA desaturase (SCD) inhibitors in a bispyrrolidine series, COA of Formula: C7H3BrClF3O, the main research area is arylheterocyclyl thiazolyltetrazoleacetic thiadiazolyltetrazoleacetic acid preparation stearoyl CoA desaturase inhibitor; arylpyrrolopyrrole isoxazolyltetrazoleacetic acid preparation stearoyl CoA desaturase inhibitor; structure arylheterocyclyl thiazolyltetrazoleacetic thiadiazolyltetrazoleacetic acid inhibition stearoyl CoA desaturase; liver selectivity pharmacokinetics thiazolyltetrazoleacetic thiadiazolyltetrazoleacetic acid stearoyl desaturase inhibitor; tissue distribution stearoyl CoA desaturase inhibitor oral administration.
Arylheterocyclyl-substituted thiazolyltetrazoleacetic acids such as I and an isoxazolyltetrazoleacetic acid and a thiadiazolyltetrazoleacetic acid are prepared as inhibitors of stearoyl-CoA desaturase (SCD) with selectivity for the liver over other organs such as the skin and eyes in which SCD inhibitors cause undesired side effects. Coupling of a mono-Boc-protected perhydropyrrolopyrrole with 2-bromo-1-chloro-4-trifluoromethoxybenzene followed by Boc deprotection yielded a salt of the arylperhydropyrrolopyrrole II (either a chloride or trifluoroacetate); amidation of Et 2-bromo-5-thiazolecarboxylate, dehydration to the nitrile, and reaction with sodium azide yielded the bromothiazolyltetrazole III. Regioselective alkylation of III with a bromoacetate ester, coupling to II, and cleavage of the ester yielded I. The inhibition of stearoyl-CoA desaturase and its inhibition in rat hepatic cells and rat cells possessing active transporters by arylheterocyclyl-substituted thiazolyltetrazoleacetic acids and thiadiazolyltetrazoleacetic acids was determined; for I and two related compounds, their tissue distributions and in vivo stearoyl-CoA desaturase inhibitions on oral administration to mice were determined
Bioorganic & Medicinal Chemistry Letters published new progress about Active biological transport. 468075-00-5 belongs to class chlorides-buliding-blocks, name is 2-Bromo-1-chloro-4-(trifluoromethoxy)benzene, and the molecular formula is C7H3BrClF3O, COA of Formula: C7H3BrClF3O.
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