Recommanded Product: Methyl 3-bromopropanoate. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: Methyl 3-bromopropanoate, is researched, Molecular C4H7BrO2, CAS is 3395-91-3, about Design, synthesis and biological evaluation of pyridyl substituted benzoxazepinones as potent and selective inhibitors of aldosterone synthase.
Exorbitant aldosterone is closely associated with various severe diseases, including congestive heart failure and chronic kidney disease. As aldosterone synthase is the pivotal enzyme in aldosterone biosynthesis, its inhibition constitutes a promising treatment for these diseases. Via a structure-based approach, a series of pyridyl substituted 3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-ones I (R = dimethylaminyl, F, pyrrolidin-1-yl, etc.; R1 = 4-methylpyridin-3-yl, 5-(trifluoromethyl)pyridin-3-yl, 5-fluoropyridin-3-yl, etc.) were designed as inhibitors of aldosterone synthase. Six compounds I (R = dimethylaminyl, R1 = 5-methylpyridin-3-yl; R1 = R = dimethylaminyl, 4-methylpyridin-3-yl; R = dimethylaminyl, R1 = 5-methoxypyridin-3-yl; R1 = 4-methylpyridin-3-yl, R = morpholin-4-yl; R1 = 4-methylpyridin-3-yl, R = piperazin-1-yl (II); R1 = 4-methylpyridin-3-yl, R = 4-methylpiperazin-1-yl) distinguished themselves with potent inhibition (IC50 <100 nmol/L) and high selectivity over homogenous 11β-hydroxylase. As the most promising compound, (II) exhibited an IC50 of 12 nmol/L and an excellent selectivity factor (SF) of 157, which are both superior to those of the reference fadrazole (IC50 = 21 nmol/L, SF = 7). Importantly, (II) showed no inhibition against steroidogenic CYP17, CYP19 and a panel of hepatic CYP enzymes indicating an outstanding safety profile. As it manifested satisfactory pharmacokinetic properties in rats, compound (II) was considered as a drug candidate for further development. The article 《Design, synthesis and biological evaluation of pyridyl substituted benzoxazepinones as potent and selective inhibitors of aldosterone synthase》 also mentions many details about this compound(3395-91-3)Recommanded Product: Methyl 3-bromopropanoate, you can pay attention to it, because details determine success or failure
Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem