Nakamura, Shinji’s team published research in Bioorganic & Medicinal Chemistry in 2022-01-15 | 401-78-5

Bioorganic & Medicinal Chemistry published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (Human RBP4 Gene). 401-78-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrF3, Recommanded Product: 3-Bromobenzotrifluoride.

Nakamura, Shinji; Kamaura, Masahiro; Akao, Yuichiro; Nakamura, Natsuko; Mizukami, Atsushi; Goto, Akihiko; Furuyama, Naoki; Cho, Nobuo; Kasai, Shizuo published the artcile< Discovery of phenylpyrrolidine derivatives as a novel class of retinol binding protein 4 (RBP4) reducers>, Recommanded Product: 3-Bromobenzotrifluoride, 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 Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (Human RBP4 Gene). 401-78-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrF3, Recommanded Product: 3-Bromobenzotrifluoride.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary