1245904-86-2Relevant academic research and scientific papers
2, 4, 5-trisubstituted selenazole class compound and its preparation method, composition and use thereof
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, (2016/11/17)
The invention relates to 2,4,5-trisubstituted selenazole compounds and a preparation method, a composition and application thereof, in particular to compounds in a formula (I), or all possible isomers, predrugs, pharmaceutically acceptable salts, solvates or hydrates thereof, wherein each substituent is shown as the description. The invention also relates to a method for preparing the compounds in the formula (I), medicinal compositions comprising the compounds in the formula (I), and application of the compounds in the formula (I) or the medicinal compositions in preparation of medicines for treating and/or preventing phospholipid transfer protein (PLTP) activity increase and/or diseases or syndromes related with the phospholipid transfer protein activity increase. The compounds in the formula (I) have good effect of inhibiting the PLTP activity and/or cholesteryl ester transfer protein (CETP) activity of blood plasma, and can be used for treating diseases on the basis.
Synthesis of a series of novel 2,4,5-trisubstituted selenazole compounds as potential PLTP inhibitors
Ling, Cui,Zheng, Zhibing,Jiang, Xian Cheng,Zhong, Wu,Li, Song
scheme or table, p. 5123 - 5125 (2010/10/19)
Based on a homology-modeled structure of PLTP and characteristic structural features of reported cholesteryl ester transfer protein (CETP) inhibitors, we designed and synthesized a novel series of 2,4,5-trisubstituted selenazole compounds. Biological evaluation reveals that compounds 12 and 17 exhibit favorable PLTP activity, and their IC50s are 8 μM and 10 μM, respectively.
