Clarke, Earl published the artcileDesign and synthesis of a potent, highly selective, orally bioavailable, retinoic acid receptor alpha agonist, Category: chlorides-buliding-blocks, the main research area is chloroethoxyisopropoxybenzamidomethylbenzoate preparation bioavailability retinoate receptor alpha agonist.
A ligand-based virtual screening exercise examining likely bioactive conformations of AM 580 and AGN 193836 was used to identify the novel, less lipophilic RARα agonist 4-(3,5-dichloro-4-ethoxybenzamido)benzoic acid (5), which has good selectivity over the RARβ, and RARγ receptors. Anal. of the medicinal chem. parameters of the 3,5-substituents of derivatives of template (5) enabled the authors to design a class of drug-like mols. with lower intrinsic clearance and higher oral bioavailability which led to the novel RARα agonist 4-(3-chloro-4-ethoxy-5-isopropoxybenzamido)-2-methylbenzoic acid (56) that has high RARα potency and excellent selectivity vs. RARβ (2 orders of magnitude) and RARγ (4 orders of magnitude) at both the human and mouse RAR receptors with improved drug-like properties. This RARα specific agonist (56) has high oral bioavailability (>80%) in both mice and dogs with a good PK profile and was shown to be inactive in cytotoxicity and genotoxicity screens.
Bioorganic & Medicinal Chemistry published new progress about Binding energy. 62936-23-6 belongs to class chlorides-buliding-blocks, name is 3-Chloro-4-hydroxy-5-methoxybenzoic acid, and the molecular formula is C8H7ClO4, Category: chlorides-buliding-blocks.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics