Synthesis and SAR study of 4, 5-diaryl-1H-imidazole-2 (3H)-thione derivatives, as potent 15-lipoxygenase inhibitors

…, M Alimardani, A Sakhteman, H Nadri, A Shafiee

文献索引：Assadieskandar, Amir; Amini, Mohsen; Salehi, Marjan; Sadeghian, Hamid; Alimardani, Maliheh; Sakhteman, Amirhossein; Nadri, Hamid; Shafiee, Abbas Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 24 p. 7160 - 7166

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被引用次数: 12

摘要

A series of 4, 5-diaryl-1H-imidazole-2 (3H)-thione was synthesized and their inhibitory potency against soybean 15-lipoxygenase and free radical scavenging activities were determined. Compound 11 showed the best IC50 for 15-LOX inhibition (IC50= 4.7 μM) and free radical scavenging activity (IC50= 14μM). Methylation of SH at C2 position of imidazole has dramatically decreased the 15-LOX inhibition and radical scavenging activity as it can ...