两种苯并咪唑类化合物对酵母的生长影响-药物化官学（医）专业毕业论文.docx

ABSTRACTAs ABSTRACT As we know,benzimidazole is important pharmaceutical intermediate．They have extensive biological activity in anti—bacterial，anti-diabetes，anti-cancer,anti-hypertensio- n，anti．parasitic，anti—ulcer,histamine receptor antagonists and protonpump inhibitor etc． We designed and synthesized 3 1 benzimidazole derivitives based on benzimidazole t- emplates．We got two type compounds through the Schiffs base and Amidmation r- eaction，respectively．All compounds were characterized by 1H-NMR and¨C-NMR．． Sir2 is an NAD+dependent deacetylase，which may mediate the effects of calorie restriction．Acfivating Sir2 deacetylase Can promote yeast growth and prolong yeast life． The natural small molecule Resveratrol Can activate Sir2 deacetylase．Yeast parental strain—BY4743 Was selected as biological activity screening model in Sir2 activator application．Therefore．we test 3 1 benzimidazole derivitives against yeast parental strain-BY4743 to search potential Sir2 activators． The results showed that Compound 5((Z)一4一(((3一(1H—benzo[d]imidazol-2-y1)phenyl) imino)methyl)一2一methoxyphen01)、Compound 6((Z)一3一(1H—benzo[d]imidazol-2一y1)-N‘(4‘ methoxybenzylidene)aniline)、Compound 14((E)一4一(1H—benzo[d]imidazol-2-y1)-N一(3一nitro benzylidene)aniline)、Compound 25(N一(4一(1H-benzo[d]imidazol一2一y1)phenyl)一2一nitrobenz‘ amide)、and Compound 29(N一(4-(5-methyl一1H—benzo-[d】imidazol-2-y1)phenyl)-2-nitroben- zamide)may also activate Sir2 deacetylase compared to RSV and the slope of the logarithmic growth of is greater than the control group RSV．The maximum OD600 value in stable period of above compounds is greater than the control resveratr01． In addition，no inhibition in the lag phase Was found．Therefore，the above Compo— und 5、Compound 6、Compound 14、Compound 25、and Compound 29 may aetiv- ate Sir2 deacetylase with a lower cytotoxicity． Keyword：Benzimidazole，Derivatives，Yeast-BY4743，Sir2，Sirtl，Biological Screening 万方数据 目 目 录 1前。言 1 1．1苯并咪唑类化合物文献概述 ．．1 1．2苯并咪唑类化合物的合成方法 ．．1 1．2．1以邻苯二胺和羧酸