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Design, synthesis, in vitro determination and molecular docking studies of 4-(1-(tert-butyl)-3-phenyl-1H-pyrazol-4-yl) pyridine derivatives with terminal sulfonamide derivatives in LPS-induced RAW264.7 macrophage cellsopen access

Authors
Mersal, Karim I.Abdel-Maksoud, Mohammed S.Ali, Eslam M. H.Ammar, Usama M.Zaraei, Seyed-OmarKim, Jae-MinKim, Su-YeonLee, Kyung-TaeLee, Kwan HyiKim, Si-WonPark, Hyun-MeeJi, Mi-JungOh, Chang-Hyun
Issue Date
10월-2021
Publisher
SPRINGER BIRKHAUSER
Keywords
Inflammation; Nitric oxide; PGE(2); COX-2; 1-(tert-butyl)-1H-pyrazole; Sulfonamide
Citation
MEDICINAL CHEMISTRY RESEARCH, v.30, no.10, pp.1925 - 1942
Indexed
SCIE
SCOPUS
Journal Title
MEDICINAL CHEMISTRY RESEARCH
Volume
30
Number
10
Start Page
1925
End Page
1942
URI
https://scholar.korea.ac.kr/handle/2021.sw.korea/144647
DOI
10.1007/s00044-021-02784-9
ISSN
1054-2523
Abstract
In the present work, a new series of 4-(1-(tert-butyl)-3-phenyl-1H-pyrazol-4-yl) pyridine possessing terminal ethyl or propyl sulfonamides was designed and synthesized. The cytotoxic effect of the final compounds was measured by applying MTT assay in LPS-Induced RAW264.7 macrophage cells. The final target compounds were screened for their anti-inflammatory effect through their ability to inhibit NO and PGE(2) production and cytokines production (TNF-alpha, IL-6, IL-1 beta) in LPS-induced RAW264.7 macrophage at 10 mu M concentration. Compounds 8d, 9d, and 9k showed the highest inhibitory effect on NO production. Compounds 8d and 9k exhibited high PGE(2) inhibition with IC50 values of 3.47, 2.54 mu M, respectively. Compounds 8d and 9k exhibited high cytokines inhibition >= 60%. The most potent compounds 8d and 9k were tested to determine their effect on iNOS and COX-2 mRNA expression level. Compound 9k activity on iNOS and COX-2 proteins level, pro-inflammatory mediators and cytokines was determined and showed remarkable inhibition for both proteins level. Compounds 8d, 9k showed high binding affinity to COX-2 active site and exhibited similar binding interactions of the native ligand celecoxib.
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