1276122-45-2Relevant academic research and scientific papers
Discovery of the selective sphingomyelin synthase 2 inhibitors with the novel structure of oxazolopyridine
Qi, Xiang-Yu,Cao, Yang,Li, Ya-Li,Mo, Ming-Guang,Zhou, Lu,Ye, De-Yong
, p. 3511 - 3515 (2017)
Sphingomyelin synthase (SMS) is a key enzyme in sphingomyelin biosynthetic pathway, whose activity is highly related to the atherosclerosis progression. SMS2 could serve as a promising therapeutic target for atherosclerosis. Based on the structure of lead compound D2, a series of oxazolopyridine derivatives were designed, synthesized, and their inhibitory activities against purified SMS1 and SMS2 enzymes were evaluated respectively. The representative molecules QY4 and QY16 possess micromolar inhibitory activities against SMS2 and excellent isoform preferences over SMS1, qualified to be selected as potential molecules in further discovery of specific SMS2 inhibitors.
2-benzyloxyphenyloxazolopyridine compound and medicinal application thereof
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Paragraph 0020, (2018/08/28)
The invention belongs to the field of medicine chemistry and relates to a 2-benzyloxyphenyloxazolopyridine compound represented as the formula (I), and a medicinal application thereof, wherein the R,X, Y and Z are coincided with details in specification. The compound can inhibit activity of sphingomyelin synthase and can be used for preparing a sphingomyelin synthase small-molecular inhibitor. The invention provides the compound represented as the formula (I) or a medicine composition employing the compound (I) as an active component, and the application of the medicine composition for preparing a medicine for preventing/treating diseases caused by abnormal increasing of sphingomyelin level, wherein the diseases include following metabolic syndromes: atherosclerosis, fatty liver, obesity,diabetes type II and the like.
Transformation of anionically activated trifluoromethyl groups to heterocycles under mild aqueous conditions
Qiao, Jennifer X.,Wang, Tammy C.,Hu, Carol,Li, Jianqing,Wexler, Ruth R.,Lam, Patrick Y. S.
supporting information; experimental part, p. 1804 - 1807 (2011/06/19)
The (hetero)aromatic trifluoromethyl group is present in many biologically active molecules and is generally considered to be chemically stable. In this paper, a convenient one-step synthesis of C-C linked aryl-heterocycles or heteroaryl-heterocycles in good to excellent yields via the reaction of anionically activated trifluoromethyl groups with amino nucleophiles containing a second NH, OH, or SH nucleophile in 1 N sodium hydroxide is reported. The method has high functional group tolerability and is potentially useful in parallel synthesis.
