Design and synthesis of fused soluble epoxide hydrolase/peroxisome proliferator-activated receptor modulators

被引：6

作者：

Bloecher, R. ^{[1
]}

Lamers, C. ^{[1
]}

Wittmann, S. K. ^{[1
]}

Diehl, O. ^{[1
]}

Hanke, T. ^{[1
]}

Merk, D. ^{[1
]}

Steinhilber, D. ^{[1
]}

Schubert-Zsilavecz, M. ^{[1
]}

Kahnt, A. S. ^{[1
]}

Proschak, E. ^{[1
]}

机构：

[1] Goethe Univ Frankfurt, Inst Pharmaceut Chem, Max von Laue Str 9, D-60438 Frankfurt, Germany

来源：

MEDCHEMCOMM | 2016年 / 7卷 / 06期

关键词：

PPAR-GAMMA; ACID-DERIVATIVES; IN-VITRO; DUAL INHIBITORS; HYDROLASE; ALPHA; DETERMINANTS; DISCOVERY; AGONIST; POTENT;

D O I：

10.1039/c6md00042h

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Metabolic syndrome (MetS) is a widespread, complex disease cluster which consists of hypertension, atherosclerosis, dyslipidaemia and type II diabetes. The treatment of MetS requires multiple pharmaceutical agents leading to complex polypharmacy. Multi-target compounds might reduce the number of required drugs in MetS patients. In this study we fused three different pharmacophores of soluble epoxide hydrolase (sEH) inhibitors and peroxisome proliferator-activated receptor (PPAR) agonists. The most promising fused scaffold exhibits multi-target activity and represents a valuable starting point for design and evaluation of fused sEH/PPAR modulators.

引用

页码：1209 / 1216

页数：8

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