COA of Formula: C3H8ClNOIn 2014 ,《Design, Synthesis, and Evaluation of Nonretinoid Retinol Binding Protein 4 Antagonists for the Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease》 appeared in Journal of Medicinal Chemistry. The author of the article were Cioffi, Christopher L.; Dobri, Nicoleta; Freeman, Emily E.; Conlon, Michael P.; Chen, Ping; Stafford, Douglas G.; Schwarz, Daniel M. C.; Golden, Kathy C.; Zhu, Lei; Kitchen, Douglas B.; Barnes, Keith D.; Racz, Boglarka; Qin, Qiong; Michelotti, Enrique; Cywin, Charles L.; Martin, William H.; Pearson, Paul G.; Johnson, Graham; Petrukhin, Konstantin. The article conveys some information:
Accumulation of lipofuscin in the retina is associated with pathogenesis of atrophic age-related macular degeneration and Stargardt disease. Lipofuscin bisretinoids (exemplified by N-retinylidene-N-retinylethanolamine) seem to mediate lipofuscin toxicity. Synthesis of lipofuscin bisretinoids depends on the influx of retinol from serum to the retina. Compounds antagonizing the retinol-dependent interaction of retinol-binding protein 4 (RBP4) with transthyretin in the serum would reduce serum RBP4 and retinol and inhibit bisretinoid formation. The authors recently showed that I, a potent carboxylic acid based RBP4 antagonist, can significantly reduce lipofuscin bisretinoid formation in the retinas of Abca4-/- mice. As part of the NIH Blueprint Neurotherapeutics Network project the authors undertook the in vitro exploration to identify novel conformationally flexible and constrained RBP4 antagonists with improved potency and metabolic stability. The authors also demonstrate that upon acute and chronic dosing in rats, II, a potent cyclopentyl fused pyrrolidine antagonist, reduced circulating plasma RBP4 protein levels by approx. 60%. The experimental part of the paper was very detailed, including the reaction process of Azetidin-3-ol hydrochloride(cas: 18621-18-6COA of Formula: C3H8ClNO)
Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.COA of Formula: C3H8ClNO Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.
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