The present invention relates to a compound of the general formula (1):
wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; R
1
is an optionally substituted alkyl group, and the like; and R
2
is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.
The present invention provides a novel compound that is structurally similar to curcumin and has a suppressive effect on Aβ aggregation, a degradative effect on Aβ aggregates, an inhibitory effect on β-secretase, and a protective effect on neurons. The novel compound is a compound represented by the following general formula (Ia) or a salt thereof:
wherein R
1
represents a 4-hydroxy-3-methoxyphenyl group or the like, and R
2
represents a 1H-indol-6-yl group or the like.
The present invention relates to a compound of the general formula (1):
wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; R
1
is an optionally substituted alkyl group, and the like; and R
2
is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.
Divergent synthesis of nitrogen heterocycles<i>via</i>H<sub>2</sub>O-mediated hydride transfer reactions
作者:Fangzhi Hu、Zhipeng Sun、Mengzhe Pan、Liang Wang、Lubin Xu、Xiong-Li Liu、Shuai-Shuai Li
DOI:10.1039/d3gc00166k
日期:——
of diverse nitrogenheterocycles from readily available feedstocks was developed by a hydride transferstrategy. A variety of 3-carboxyl and 3-acyl substituted tetrahydroquinolines and 3,4-dihydroquinolin-2(1H)-ones were obtained via cascade Knoevenagel condensation/[1,5]-hydride transfer/cyclization/hydrolysis/decarboxylation and cascade Knoevenagel condensation/[1,5]-hydride transfer/N-dealkylation/N-acylation
通过氢化物转移策略开发了H 2 O 促进的多种氮杂环化合物从现成原料的可控合成。通过级联Knoevenagel缩合/[ 1,5 ]-氢化物转移/环化/水解/脱羧和级联Knoevenagel获得了多种3-羧基和3-酰基取代的四氢喹啉和3,4-二氢喹啉-2(1 H) -ones分别为缩合/[1,5]-氢化物转移/ N-脱烷基化/ N-酰化过程。此外,还很好地介绍了方法学和机理研究的综合效用。
TRISUBSTITUTED AMINE COMPOUNDS AS INHIBITORS OF -CHOLESTERYL ESTER TRANSFER PROTEIN CETP