68524-17-4Relevant academic research and scientific papers
A practical synthesis for (S)-5-(4-(1-methylethoxy)phenyl)-5-methylimidazolidine-2,4-dione and its application in the synthesis of a novel liver X receptor β-selective agonist
Koura, Minoru,Sumida, Hisashi,Yamazaki, Yukiyoshi,Shibuya, Kimiyuki
, p. 63 - 68 (2015/12/31)
In this manuscript, the chiral separation of novel liver X receptor (LXR) β-selective agonist (±)-1 revealed that (S)-5-(4-(1-methylethoxy)phenyl)-5-methylimidazolidine-2,4-dione (+)-2 was the essential moiety (tail) to express LXR β-selective agonistic a
Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists
Koura, Minoru,Matsuda, Takayuki,Okuda, Ayumu,Watanabe, Yuichiro,Yamaguchi, Yuki,Kurobuchi, Sayaka,Matsumoto, Yuuki,Shibuya, Kimiyuki
, p. 2668 - 2674 (2015/06/08)
A novel series of 1,3-bistrifluoromethylcarbinol derivatives that act as liver X receptor (LXR) β-selective agonists was discovered. Structure-activity relationship studies led to the identification of molecule 62, which was more effective (Emax) and selective toward LXRβ than T0901317 and GW3965. Furthermore, 62 decreased LDL-C without elevating the plasma TG level and significantly suppressed the lipid-accumulation area in the aortic arch in a Bio F1B hamster fed a diet high in fat and cholesterol. We demonstrated that our LXRβ agonist would be potentially useful as a hypolipidemic and anti-atherosclerotic agent. In this manuscript, we report the design, synthesis and pharmacology of 1,3-bistrifluoromethylcarbinol derivatives.
CARBINOL DERIVATIVES HAVING HETEROCYCLIC LINKER
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Page/Page column 15, (2010/12/29)
[Object] It is to provide a novel LXRβ agonist useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate: (wherein, each V and W independently show N or C—R7; each X and Y independently show CH2, C═O, SO2, etc; Z shows CH or N; each R1, R2 and R7 independently show a hydrogen atom, C1-8 alkyl group, etc.; R3 shows C1-8 alkyl group; R4 shows an optionally substituted C6-10 aryl group or an optionally substituted 5- to 11-membered heterocyclic group; R5 and R6 show a hydrogen atom, etc.; L shows a C1-8 alkyl chain optionally substituted with an oxo group, etc.; and n shows any integer of 0 to 2.)
CARBINOL DERIVATIVES HAVING CYCLIC LINKER
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Page/Page column 20, (2010/03/31)
[Object] To provide a novel LXRβ agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate.
