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Design and synthesis of dual modulators of soluble epoxide hydrolase and peroxisome proliferator-activated receptors

la Buscató, Estel and Blöcher, René and Lamers, Christina and Klingler, Franca-Maria and Hahn, Steffen and Steinhilber, Dieter and Schubert-Zsilavecz, Manfred and Proschak, Ewgenij. (2012) Design and synthesis of dual modulators of soluble epoxide hydrolase and peroxisome proliferator-activated receptors. Journal of Medicinal Chemistry, 55 (23). pp. 10771-10775.

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Official URL: https://edoc.unibas.ch/70333/

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Abstract

Metabolic syndrome is a complex condition which often requires the use of multiple medications as a treatment. The resulting problems of polypharmacy are increase in side effects, drug-drug interactions, and its high economic cost. Development of multitarget compounds is a promising strategy to avoid the complications arising from administration of multiple drugs. Modulators of peroxisome proliferator-activated receptors (PPARs) are established agents in the treatment of dyslipidaemia, hyperglycaemia, and insulin resistance. Inhibitors of soluble epoxide hydrolase (sEH) are under evaluation for their use in cardiovascular diseases. In the present study, a series of dual sEH/PPAR modulators containing a pyrrole acidic headgroup and a urea pharmacophore were designed, synthesized, and evaluated in vitro using recombinant enzyme and cell-based assays. Compounds with different activity profiles were obtained which could be used in the treatment of metabolic syndrome.
Faculties and Departments:05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Molekulare Pharmazie (Ricklin)
UniBasel Contributors:Lamers, Christina
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:American Chemical Society
ISSN:0022-2623
e-ISSN:1520-4804
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:16 Nov 2020 11:03
Deposited On:16 Nov 2020 11:03

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