A spectrofluorimetric method for the direct analysis of carbendazim [methyl 2-benzimidazole carbamate (MBC)] fungicide and its metabolite 2-aminobenzimidazole (2-AB) in natural waters is described. Very low limit of d...A spectrofluorimetric method for the direct analysis of carbendazim [methyl 2-benzimidazole carbamate (MBC)] fungicide and its metabolite 2-aminobenzimidazole (2-AB) in natural waters is described. Very low limit of detection (LOD) and limit of quantification (LOQ) values of 0.002 - 0.06 ng/mL and 0.006 - 0.2 ng/mL, respectively, were determined by spectrofluorimetric method with small relative standard deviation (RSD) values < 1%. This spectrofluorimetric method was applied to the determination of MBC and 2-AB residues in natural waters, with satisfactory recovery values of (88.5% - 119.2%).展开更多
Fragment-based drug discovery （FBDD） has been widely applied in the research of aspartyl protease inhibitors. In the present study, we reported our work on 2-aminobenzimidazole as the original fragment, which was pr...Fragment-based drug discovery （FBDD） has been widely applied in the research of aspartyl protease inhibitors. In the present study, we reported our work on 2-aminobenzimidazole as the original fragment, which was predicted to bind with the catalytic aspartyl dyad （Asp228 and Asp32） of D-site amyloid precursor protein cleaving enzyme 1 （BACE1）. A series of novel 2-aminobenzimidazole derivatives were designed and synthesized. The results from FRET assay revealed that three out of the 12 designed 2-aminobenzimidazoles could inhibit more than 50% of the enzymatic potency of BACE1 at 10 pM. Docking study showed that 2-aminobenzimidazole could form multiple hydrogen bonds and occupy S1/$2＇ pockets well.展开更多
基金the Service of Cooperation and Cultural Action of the Embassy of France for financial support
文摘A spectrofluorimetric method for the direct analysis of carbendazim [methyl 2-benzimidazole carbamate (MBC)] fungicide and its metabolite 2-aminobenzimidazole (2-AB) in natural waters is described. Very low limit of detection (LOD) and limit of quantification (LOQ) values of 0.002 - 0.06 ng/mL and 0.006 - 0.2 ng/mL, respectively, were determined by spectrofluorimetric method with small relative standard deviation (RSD) values < 1%. This spectrofluorimetric method was applied to the determination of MBC and 2-AB residues in natural waters, with satisfactory recovery values of (88.5% - 119.2%).
基金National Natural Science Foundation of China(Grant No.21002002/21172012)
文摘Fragment-based drug discovery （FBDD） has been widely applied in the research of aspartyl protease inhibitors. In the present study, we reported our work on 2-aminobenzimidazole as the original fragment, which was predicted to bind with the catalytic aspartyl dyad （Asp228 and Asp32） of D-site amyloid precursor protein cleaving enzyme 1 （BACE1）. A series of novel 2-aminobenzimidazole derivatives were designed and synthesized. The results from FRET assay revealed that three out of the 12 designed 2-aminobenzimidazoles could inhibit more than 50% of the enzymatic potency of BACE1 at 10 pM. Docking study showed that 2-aminobenzimidazole could form multiple hydrogen bonds and occupy S1/$2＇ pockets well.
