867262-56-4Relevant academic research and scientific papers
Synthesis and structure-activity relationships of N-(4-amino-2,6-diisopropylphenyl)-N'-(1,4-diarylpiperidine-4-yl)methylureas as anti-hyperlipidemic agents
Asano, Shigehiro,Ban, Hitoshi,Kino, Koichi,Ioriya, Katsuhisa,Muraoka, Masami
experimental part, p. 4636 - 4646 (2009/10/23)
Based on 1,4-diarylpiperidine-4-methylureas, a new class of ACAT inhibitors, we examined in the study the SAR of a series of compounds prepared by replacing the substituent at the three aromatic parts. Introduction of long alkoxy group onto the phenyl moi
Novel 1,4-diarylpiperidine-4-methylureas as anti-hyperlipidemic agents: Dual effectors on acyl-CoA:cholesterol O-acyltransferase and low-density lipoprotein receptor expression
Asano, Shigehiro,Ban, Hitoshi,Kino, Kouichi,Ioriya, Katsuhisa,Muraoka, Masami
scheme or table, p. 1062 - 1065 (2009/08/07)
A family of 1,4-diarylpiperidine-4-methylureas were designed and synthesized as novel dual effectors on ACAT and LDL receptor expression. We examined SAR of the synthesized compounds focusing on substitution at the three aromatic parts of the starting compound 1 and succeeded in identifying essential substituents for inhibition of ACAT and up-regulation of hepatic LDL receptor expression. Especially, we found that compound 12f, which can easily be prepared, has biological properties comparable to those of SMP-797, a promising ACAT inhibitor. In addition, the in vitro effects of 12f on lipid metabolism were substantially superior to those of a known ACAT inhibitor, Avasimibe.
A convenient one-pot preparation of N-substituted 4-phenylpiperidines
Asano, Shigehiro,Ban, Hitoshi
, p. 183 - 188 (2008/09/20)
N-Substituted 4-phenylpiperidines were readily synthesized by one-pot cyclization of diols with amines via bis-triflate intermediates. The new synthesis under mild conditions gave various N-substituted 4-phenylpiperidines in moderate to good yields.
NOVEL SULFONAMIDE DERIVATIVE
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Page/Page column 49, (2010/11/25)
A compound of the formula (1): wherein m, n and p is independently an integer of 0 to 4 with the proviso that 3 a?| m + n a?| 8; X is the formula: NR4, etc.; R1, R3 and R4 are a substituted or unsubstituted aryl group, etc.; R2 is a hydrogen atom, etc.; a, b, c, d, e and f are a hydrogen atom or a substituted or unsubstituted alkyl group, etc.; Y is the formula: -SO2-, etc.; and Z is an oxygen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt of the same has an activity of potentiating an expression of a low density lipoprotein receptor and thus is useful as an agent for treating hyperlipidemia or arteriosclerosis.
