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https://hdl.handle.net/20.500.11851/10366
Title: | Synthesis of Some Piperazine/Piperidine Amides of Chromone-2 Carboxylic Acid as Potential Soluble Epoxide Hydrolase (seh) Inhibitors | Authors: | Gür Maz, Tuğçe Çalışkan, Huseyin Burak |
Keywords: | Fluorometric inhibition piperazine piperidine soluble epoxide hydrolase ?2023 ACG Publication All right reserved Insights Target |
Publisher: | Acg Publications | Abstract: | Inhibition of soluble epoxide hydrolase (sEH) is implicated as a new therapeutic approach against inflammatory disorders in the context of metabolic and cardiovascular diseases. In the course of our ongoing research on sEH inhibitors, we synthesized novel piperidine/piperazine amide derivatives of the chromone-2-carboxylic acid, and evaluated their inhibitory properties against human sEH. The chemical structures of the target compounds (2-5, 79) were elucidated by means of 1H-NMR, 13C-NMR and HRMS spectra. Initial screening of final compounds against sEH at a final concentration of 10 .M led to the identification of compound 7, which inhibited sEH activity in a concentration-dependent manner with an IC50 = 1.75 .M. Therefore, this chromone-2-amide derivative 7 decorated with benzyl piperidine on the amide side can be regarded as a novel lead structure, which pave the way of developing new analogues with improved inhibitory activities against sEH. | URI: | https://doi.org/10.25135/acg.oc.145.2302.2705 https://hdl.handle.net/20.500.11851/10366 |
ISSN: | 1307-6175 |
Appears in Collections: | Scopus İndeksli Yayınlar Koleksiyonu / Scopus Indexed Publications Collection WoS İndeksli Yayınlar Koleksiyonu / WoS Indexed Publications Collection |
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