Nakamura, Shinji published the artcileDiscovery of phenylpyrrolidine derivatives as a novel class of retinol binding protein 4 (RBP4) reducers, Category: alcohols-buliding-blocks, the main research area is trifluoromethyl phenyl oxazolyl propanoic acid preparation RBP4 reducer SAR; pyrrolidinyloxy acetic acid trifluoromethyl phenyl preparation RBP4 reducer SAR; Age-related macular degeneration (AMD); Diabetes; Protein–protein interaction (PPI); Retinol-binding protein 4 (RBP4); Transthyretin (TTR).
Retinol-binding protein 4 (RBP4) is a potential drug target for metabolic and ophthalmol. diseases. A high-throughput screening of compound library has identified a small-mol. RBP4 reducer compound I, as a hit compound Aiming to provide a suitable tool for investigating the pharmacol. effects of RBP4 reducers, we conducted a structure-activity relationship study of compound I. Exploration of the aryl head, oxazole core, and propanoic acid tail of compound I resulted in the discovery of novel, potent, and orally available phenylpyrrolidine derivatives ({(3S)-1-[3,5-bis(trifluoromethyl)phenyl]pyrrolidin-3-yl}oxy)acetic acid and ({(3R)-1-[3,5-bis(trifluoromethyl)phenyl]pyrrolidin-3-yl}oxy)acetic acid. Compound ({(3S)-1-[3,5-bis(trifluoromethyl)phenyl]pyrrolidin-3-yl}oxy)acetic acid had a potent and long-lasting blood RBP4-level-reducing effect when orally administered to mice at a dose as low as 0.3 mg/kg.
Bioorganic & Medicinal Chemistry published new progress about Eye disease. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Category: alcohols-buliding-blocks.
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