COA of Formula: C3H8ClNOIn 2015 ,《Discovery of an Oral Respiratory Syncytial Virus (RSV) Fusion Inhibitor (GS-5806) and Clinical Proof of Concept in a Human RSV Challenge Study》 appeared in Journal of Medicinal Chemistry. The author of the article were Mackman, Richard L.; Sangi, Michael; Sperandio, David; Parrish, Jay P.; Eisenberg, Eugene; Perron, Michel; Hui, Hon; Zhang, Lijun; Siegel, Dustin; Yang, Hai; Saunders, Oliver; Boojamra, Constantine; Lee, Gary; Samuel, Dharmaraj; Babaoglu, Kerim; Carey, Anne; Gilbert, Brian E.; Piedra, Pedro A.; Strickley, Robert; Iwata, Quynh; Hayes, Jaclyn; Stray, Kirsten; Kinkade, April; Theodore, Dorothy; Jordan, Robert; Desai, Manoj; Cihlar, Tomas. The article conveys some information:
GS-5806 I is a novel, orally bioavailable RSV fusion inhibitor discovered following a lead optimization campaign on a screening hit. The oral absorption properties were optimized by converting to the pyrazolo[1,5-a]-pyrimidine heterocycle, while potency, metabolic, and physicochem. properties were optimized by introducing the para-chloro and aminopyrrolidine groups. A mean EC50 = 0.43 nM was found toward a panel of 75 RSV A and B clin. isolates and dose-dependent antiviral efficacy in the cotton rat model of RSV infection. Oral bioavailability in preclin. species ranged from 46 to 100%, with evidence of efficient penetration into lung tissue. In healthy human volunteers exptl. infected with RSV, a potent antiviral effect was observed with a mean 4.2 log10 reduction in peak viral load and a significant reduction in disease severity compared to placebo. In conclusion, a potent, once daily, oral RSV fusion inhibitor with the potential to treat RSV infection in infants and adults is reported. After reading the article, we found that the author used 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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