Benzimidazole derivative, preparation method and application thereof

The invention discloses a benzimidazole derivative shown as general formula I or pharmaceutically acceptable salts thereof, a preparation method and application thereof as a selective retinal dehydrogenase inhibitor. Specifically, R1 is selected from C1-C8 alkyl, C2-C8 alkenyl, cycloalkyl methyl or...

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Bibliographische Detailangaben
Hauptverfasser: LIANG DAILIN, LIU XIAODONG, LI BINGYAN, JIANG LING, JIANG CHENG, LIU LI
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a benzimidazole derivative shown as general formula I or pharmaceutically acceptable salts thereof, a preparation method and application thereof as a selective retinal dehydrogenase inhibitor. Specifically, R1 is selected from C1-C8 alkyl, C2-C8 alkenyl, cycloalkyl methyl or benzyl; the cycloalkyl is a 3-6-membered cycloalkyl; the benzyl can optionally be substituted by oneor more of the following groups: halogen, C1-C4 alkyl, C1-C4 alkoxy, or CF3. Compared with the prior art, the invention discloses abenzimidazole derivative and pharmaceutically acceptable salts thereof with a selective inhibition effect on retinal dehydrogenase (ALDH1A1). And pharmacological experiments prove that the compounds have a remarkable inhibition effect on ALDH1A1 and particularly can be used as diabetes treatment drugs. 本发明公开了一种通式I所示的苯并咪唑衍生物或其药学上可接受的盐,及其制备方法和其作为选择性视黄醛脱氢酶抑制剂的应用。其中,R选自C1-C8烷基、C2-C8烯基、环烷基甲基或苄基;所述环烷基为3-6元环烷基;所述苄基上可任选地被一个或多个以下基团取代:卤素、C1-C4烷基、C1-C4烷氧基或CF。相对于现有技术,本发明公开了一类对视黄醛脱氢酶(ALDH1A1)有选择性抑制作用的