Journal
MOLECULES
Volume 26, Issue 20, Pages -Publisher
MDPI
DOI: 10.3390/molecules26206093
Keywords
1,5-diarylimidazole; halogenation; COX-2; PGE(2) production; anti-inflammatory
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A series of halogenated 1,5-diarylimidazole compounds were synthesized and evaluated for their inhibitory effects on PGE(2) production. 4-halogenated 5-aryl-1-(4-methylsulfonylphenyl)imidazoles showed strong inhibitory activities regardless of halogen type, with compounds 3 and 13 exhibiting the best results.
A series of halogenated 1,5-diarylimidazole compounds were synthesized and their inhibitory effects on LPS-induced PGE(2) production in RAW 264.7 cells were evaluated. A wide variety of 2,4-, 4-, and 2-halogenated 5-aryl-1-(4-methylsulfonylphenyl)imidazoles were synthesized for SAR study via two different pathways. Overall, 4-halogenated 5-aryl-1-(4-methylsulfonylphenyl)imidazoles, regardless of the species of halogen, exhibited very strong inhibitory activities of PGE(2) production. Among them, 4-chloro-5-(4-methoxyphenyl)-1-(4-methylsulfonylphenyl)imidazole (3, IC50 3.3 nM +/- 2.93), and 4-chloro-5-(4-chlorophenyl)-1-(4-methylsulfonylphenyl)imidazole (13, IC50 5.3 nM & PLUSMN; 0.23) showed the best results.
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