In 2017,Wang, Xinran; Lin, Xuehua; Xu, Xuanqi; Li, Wei; Hao, Lijuan; Liu, Chunchi; Zhao, Dongmei; Cheng, Maosheng published 《Design, synthesis, and biological evaluation of N,N-disubstituted-4-arylthiazole-2-methylamine derivatives as cholesteryl ester transfer inhibitors》.Molecules published the findings.Reference of Ethyl 2-amino-2-thioxoacetate The information in the text is summarized as follows:
Cholesteryl ester transfer protein (CETP) has been identified as a potential target for cardiovascular disease (CVD) for its important role in the reverse cholesteryl transfer (RCT) process. In the previous work, compound I was discovered as a moderate CETP inhibitor. The replacement of the amide linker of compound I by heterocyclic aromatics a series of N,N-substituted-4-arylthiazole-2-methylamine derivatives II (R1 = 3-OMe, 3-OCF3, 4-Ph, etc.; R2 = H, 4-F, 4-NO2, etc.) were designed by utilizing a conformational restriction strategy. Thirty-six compounds were synthesized and evaluated for their CETP inhibitory activities. Structure-activity relationship studies indicate that electron donor groups substituted ring A, and electron-withdrawing groups at the 4-position of ring B were critical for potency. Among these compounds, II (R1 = 3,4-(OMe)2; R2 = 4-NO2) exhibited excellent CETP inhibitory activity (IC50 = 0.79 +/- 0.02 μM) in vitro and showed an acceptable metabolic stability. The experimental process involved the reaction of Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Reference of Ethyl 2-amino-2-thioxoacetate)
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.Reference of Ethyl 2-amino-2-thioxoacetate
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