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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
soluble epoxide hydrolase
?2023 ACG Publication
All right reserved
Issue Date: 2023
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.
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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