卤代 1,5-二芳基咪唑的合成及其对 LPS 诱导 RAW 264.7 细胞 PGE 产生的抑制作用。
Synthesis of Halogenated 1,5-Diarylimidazoles and Their Inhibitory Effects on LPS-Induced PGE Production in RAW 264.7 Cells.
机构信息
College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China.
College of Pharmacy, Kyung Hee University, Seoul 02453, Korea.
出版信息
Molecules. 2021 Oct 9;26(20):6093. doi: 10.3390/molecules26206093.
A series of halogenated 1,5-diarylimidazole compounds were synthesized and their inhibitory effects on LPS-induced PGE 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 production. Among them, 4-chloro-5-(4-methoxyphenyl)-1-(4-methylsulfonylphenyl)imidazole (, IC 3.3 nM ± 2.93), and 4-chloro-5-(4-chlorophenyl)-1-(4-methylsulfonylphenyl)imidazole (, IC 5.3 nM ± 0.23) showed the best results.
一系列卤代 1,5-二芳基咪唑化合物被合成，并评估了它们对 RAW 264.7 细胞中 LPS 诱导的 PGE 产生的抑制作用。通过两种不同的途径，合成了广泛的 2,4-、4-和 2-卤代 5-芳基-1-(4-甲基磺酰基苯基)咪唑，以进行 SAR 研究。总体而言，无论卤素的种类如何，4-卤代 5-芳基-1-(4-甲基磺酰基苯基)咪唑都表现出非常强的 PGE 产生抑制活性。其中，4-氯-5-(4-甲氧基苯基)-1-(4-甲基磺酰基苯基)咪唑（,IC 3.3 nM ± 2.93）和 4-氯-5-(4-氯苯基)-1-(4-甲基磺酰基苯基)咪唑（,IC 5.3 nM ± 0.23）表现出最佳效果。
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