The invention provides a compound shown as a formula I, or a conformational isomer thereof, or an optical isomer thereof, or a pharmaceutically acceptable salt thereof. The compound can be tightly combined with related binding proteins in an miRNA biosynthesis process and can effectively inhibit the synthesis of miRNA-21. The prepared active compound provided by the invention can be used as an miRNA-21 inhibitor, and further as a potential drug for treating malignant tumors. The formula I is shown in the description.
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Paragraph 0130; 0131; 0234-0236
(2019/06/12)
(2-Aryl-5-methylimidazol-4-ylcarbonyl)guanidines and (2-aryl-5-methyloxazol-4-ylcarbonyl)guanidines as NHE-1 inhibitors
A series of (2-aryl-5-methylimidazol-4-ylcarbonyl)guanidines and (2-aryl-5-methyloxazol-4-ylcarbonyl)guanidines were synthesized and evaluated as NHE-1 inhibitors. The structure-activity relationships well matched those of furan derivatives, which were previously investigated. The (2,5-disubstituted)phenyl compounds showed better activities than the other analogues in both imidazole and oxazole compounds. Especially, 2-(2,5-dichlorophenyl)imidazole 52, and 2-(2-methoxy-5-chlorophenyl)imidazole 54 compounds exhibited potent cardioprotective efficacy both in vitro and in vivo as well as high NHE-1 inhibitory activities.