The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: Methyl 3-bromopropanoate( cas:3395-91-3 ) is researched.Related Products of 3395-91-3.Zhu, Haichao; Liu, Meihua; Li, Haiyan; Guan, Ting; Zhang, Qi; Chen, Yang; Liu, Yingxiang; Hartmann, Rolf R.; Yin, Lina; Hu, Qingzhong published the article 《Design, synthesis and biological evaluation of pyridyl substituted benzoxazepinones as potent and selective inhibitors of aldosterone synthase》 about this compound( cas:3395-91-3 ) in Chinese Chemical Letters. Keywords: pyridyl benzoxazepinone preparation aldosterone synthase inhibitor mol docking. Let’s learn more about this compound (cas:3395-91-3).
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. If you want to learn more about this compound(Methyl 3-bromopropanoate)Related Products of 3395-91-3, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(3395-91-3).
Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem