The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 6-Acetylbenzo[d]oxazol-2(3H)-one( cas:54903-09-2 ) is researched.Recommanded Product: 6-Acetylbenzo[d]oxazol-2(3H)-one.Meyers, Marvin J.; Arhancet, Graciela B.; Hockerman, Susan L.; Chen, Xiangyang; Long, Scott A.; Mahoney, Matthew W.; Rico, Joseph R.; Garland, Danny J.; Blinn, James. R.; Collins, Joe T.; Yang, Shengtian; Huang, Horng-Chih; McGee, Kevin F.; Wendling, Jay M.; Dietz, Jessica D.; Payne, Maria A.; Homer, Bruce L.; Heron, Marcia I.; Reitz, David B.; Hu, Xiao published the article 《Discovery of (3S,3aR)-2-(3-Chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic Acid (PF-3882845), an Orally Efficacious Mineralocorticoid Receptor (MR) Antagonist for Hypertension and Nephropathy》 about this compound( cas:54903-09-2 ) in Journal of Medicinal Chemistry. Keywords: mineralocorticoid receptor antagonist benzoindazole derivative hypertension nephropathy. Let’s learn more about this compound (cas:54903-09-2).
We have discovered a novel class of nonsteroidal pyrazoline antagonists of the mineralocorticoid receptor (MR) that show excellent potency and selectivity against other nuclear receptors. Early analogs were poorly soluble and had a propensity to inhibit the hERG channel. Remarkably, both of these challenges were overcome by incorporation of a single carboxylate moiety. Structural modification of carboxylate-containing lead R-4g with a wide range of substituents at each position of the pyrazoline ring resulted in R-12o, which shows excellent activity against MR and reasonable pharmacokinetic profile. Introduction of conformational restriction led to a novel series characterized by exquisite potency and favorable steroid receptor selectivity and pharmacokinetic profile. Oral dosing of 3S,3aR-27d (PF-3882845) in the Dahl salt sensitive preclin. model of salt-induced hypertension and nephropathy showed blood pressure attenuation significantly greater than that with eplerenone, reduction in urinary albumin, and renal protection. As a result of these findings, 3S,3aR-27d was advanced to clin. studies.
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Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics