The Effect Of Two Kinds Of Benzimidazole Compounds On The Growth Of Yeast

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 31 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 by1H-NMR and 13C-NMR.Sir2 is an NAD+dependent deacetylase, which may mediate the effects of calorie restriction. Activating 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 31 benzimidazole derivitives against yeast parental strain-BY4743 to search potential Sir2 activators.The results showed that Compound 5((Z)-4-(((3-(1H-benzo[d]imidazol-2-yl)phenyl) imino)methyl)-2-methoxyphenol、Compound 6((Z)-3-(1H-benzo[d]imidazol-2-yl)-N-(4-methoxybenzylidene)aniline)、Compound 14((E)-4-(1H-benzo[d]imidazol-2-yl)-N-(3-nitro benzylidene)aniline)、Compound 25(N-(4-(1H-benzo[d]imidazol-2-yl)phenyl)-2-nitrobenz-amide)、and Compound 29(N-(4-(5-methyl-lH-benzo[d]imidazol-2-yl)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 resveratrol. 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 activ-ate Sir2 deacetylase with a lower cytotoxicity.