A series of granular activated carbons (GACs) were prepared by briquetting method from Chinese coals of different ranks and their blends, with coal pitch as the binder. Pore structural parameters including BET speci...A series of granular activated carbons (GACs) were prepared by briquetting method from Chinese coals of different ranks and their blends, with coal pitch as the binder. Pore structural parameters including BET specific surface area (SBEr), total pore volume (Vr) and average pore diameter (da) were measured and cal- culated as well as process parameters such as yield of char (CY) and burn-off (B). The relationship between the pore structural parameters of the GAC from coal blend (BC-GAC) and the ones of the GACs from corresponding single coals (SC-GACs) was analyzed, in which an index, the relative error (δ), was presented to define the bias between fitted values and experimental values of these parameters of the BC-GACs. The results show that the BC-GAC keeps qualitatively the pore structural features of the SC-GACs; as concerned as the quantitative relationship, the pore structural parameters of the BC-GAC from coal blend consisting of non-caking coals can be obtained by adding proportionally the pore structural parameters of the SC-GACs with a less than 10%. Meanwhile, for the BC-GAC from coal blend containing weak caking bituminous coal, the δ increases up to 25% and the experimental pore size distribution differs greatly from the fitted one.展开更多
According to the chemical and mineral composition characteristics of the fly ash,alumina can be extracted from fly ash through the calcining method by using sodium carbonate and calcium carbonate additives.The effects...According to the chemical and mineral composition characteristics of the fly ash,alumina can be extracted from fly ash through the calcining method by using sodium carbonate and calcium carbonate additives.The effects on leaching rate of alumina have been investigated. The results showed that the fly ash can be activated effectively and the leaching rate of alumina can be improved to more than 92% through this method. The best process parameters were the ratio of raw materials,i. e. the material weight ratio of fly ash,calcium carbonate and sodium carbonate was 1. 0∶1. 2∶0. 9. The activating temperature was 850℃-900℃,activating time was 3 h. This process has a potential application prospect and improves the value of comprehensive utilization of fly ash.展开更多
Thiazolidinediones(TZDs),such as rosiglitazone(RSG),which activates peroxisome proliferator activated receptor-y(PPARy),are a potent class of oral antidiabetic agents with good durability.However,the clinical use of T...Thiazolidinediones(TZDs),such as rosiglitazone(RSG),which activates peroxisome proliferator activated receptor-y(PPARy),are a potent class of oral antidiabetic agents with good durability.However,the clinical use of TZDs is challenging because of their side effects,including weight gain and hepatotoxicity.Here,we found that bavachinin(BVC),a lead natural product,additively activates PPARγ with lowdose RSG to preserve the maximum antidiabetic effects while reducing weight gain and hepatotoxicity in db/db mice caused by RSG monotherapy.Structural and biochemical assays demonstrated that an unexplored hotspot around Met329 and Ser332 in helix 5 is triggered by BVC cobinding to RSG-bound PPARy,thereby allosterically stabilizing the active state of the activation-function 2 motif responsible for additive activation with RSG.Based on this hotspot,we discovered a series of new classes of allosteric agonists inducing the activity of TZDs in the same manner as BVC.Together,our data illustrate that the hotspot of PPARγ is druggable for the discovery of new allosteric synergists,and the combination thera py of allosteric synergists and TZD drugs may provide a potential alternative approach to the treatment of type 2 diabetes mellitus.展开更多
N-Alkylated benzimidazole derivatives have been synthesized via the aza-Michael addition reactions of1H-benzimidazoles to a,b-unsaturated compounds in water and palladium acetate obviously promoted these transformatio...N-Alkylated benzimidazole derivatives have been synthesized via the aza-Michael addition reactions of1H-benzimidazoles to a,b-unsaturated compounds in water and palladium acetate obviously promoted these transformations. The reported method, overcoming the inactivation of palladium under the equivalent nitrogenous conditions, has the advantages of convenient manipulation, atom-economy, as well as environmental friendliness. The bioactive results showed that butyl 3-(5,6-dimethyl-1Hbenzo[d]imidazol-1-yl)propanoate(3c) exhibited excellent inhibitory activity against Bacillus subtilis(MIC = 16 mg/m L) and Bacillus proteus(MIC = 8 mg/m L). Therefore, this process would facilitate the construction of various potential bioactive compounds based on the benzimidazole scaffold under mild conditions.展开更多
A series of novel bridged-neonicotinoid analogues were designed and synthesized, which were constructed by starting material 8 with cyclopentenone or cyclohexenone in the presence of catalyst aluminium chloride. All o...A series of novel bridged-neonicotinoid analogues were designed and synthesized, which were constructed by starting material 8 with cyclopentenone or cyclohexenone in the presence of catalyst aluminium chloride. All of the compounds were characterized and confirmed by^1H NMR,^(13)C NMR, HRMS and IR. The bioassay tests showed that compounds 5 and 6a showed higher bioactivities than imidacloprid against Aphis craccivora.展开更多
基金financially supported by the National High-Tech Research and Development Program of China (No.2008AA05Z308)the National Natural Science Foundation of China (No.20776150)
文摘A series of granular activated carbons (GACs) were prepared by briquetting method from Chinese coals of different ranks and their blends, with coal pitch as the binder. Pore structural parameters including BET specific surface area (SBEr), total pore volume (Vr) and average pore diameter (da) were measured and cal- culated as well as process parameters such as yield of char (CY) and burn-off (B). The relationship between the pore structural parameters of the GAC from coal blend (BC-GAC) and the ones of the GACs from corresponding single coals (SC-GACs) was analyzed, in which an index, the relative error (δ), was presented to define the bias between fitted values and experimental values of these parameters of the BC-GACs. The results show that the BC-GAC keeps qualitatively the pore structural features of the SC-GACs; as concerned as the quantitative relationship, the pore structural parameters of the BC-GAC from coal blend consisting of non-caking coals can be obtained by adding proportionally the pore structural parameters of the SC-GACs with a less than 10%. Meanwhile, for the BC-GAC from coal blend containing weak caking bituminous coal, the δ increases up to 25% and the experimental pore size distribution differs greatly from the fitted one.
文摘According to the chemical and mineral composition characteristics of the fly ash,alumina can be extracted from fly ash through the calcining method by using sodium carbonate and calcium carbonate additives.The effects on leaching rate of alumina have been investigated. The results showed that the fly ash can be activated effectively and the leaching rate of alumina can be improved to more than 92% through this method. The best process parameters were the ratio of raw materials,i. e. the material weight ratio of fly ash,calcium carbonate and sodium carbonate was 1. 0∶1. 2∶0. 9. The activating temperature was 850℃-900℃,activating time was 3 h. This process has a potential application prospect and improves the value of comprehensive utilization of fly ash.
基金the National Natural Science Foundation of China(21708025,81925034,91753117,and 81773793)the Open Fund of State Key Laboratory of Oncogenes and Related Genes,Shanghai Jiao Tong University School of Medicine+3 种基金the Innovation Program of Shanghai Municipal Education Commission(2019-01-07-00-01-E00036)the Shanghai Science and Technology Innovation Foundation(19431901600)the China Postdoctoral Science Foundation(2016M601618 and 2017T100303)the National Science and Technology Major Project of China(2018ZX09711001-005-022)。
文摘Thiazolidinediones(TZDs),such as rosiglitazone(RSG),which activates peroxisome proliferator activated receptor-y(PPARy),are a potent class of oral antidiabetic agents with good durability.However,the clinical use of TZDs is challenging because of their side effects,including weight gain and hepatotoxicity.Here,we found that bavachinin(BVC),a lead natural product,additively activates PPARγ with lowdose RSG to preserve the maximum antidiabetic effects while reducing weight gain and hepatotoxicity in db/db mice caused by RSG monotherapy.Structural and biochemical assays demonstrated that an unexplored hotspot around Met329 and Ser332 in helix 5 is triggered by BVC cobinding to RSG-bound PPARy,thereby allosterically stabilizing the active state of the activation-function 2 motif responsible for additive activation with RSG.Based on this hotspot,we discovered a series of new classes of allosteric agonists inducing the activity of TZDs in the same manner as BVC.Together,our data illustrate that the hotspot of PPARγ is druggable for the discovery of new allosteric synergists,and the combination thera py of allosteric synergists and TZD drugs may provide a potential alternative approach to the treatment of type 2 diabetes mellitus.
基金supported by the National Natural Science Foundation of China(Nos.21004075,21372186)Beijing National Laboratory of Molecular Sciences(BNLMS)(No.20140130)+1 种基金the Doctoral Fund of Southwest University(No.SWU111075)the Research Funds for the Central Universities(No.XDJK2013C112)
文摘N-Alkylated benzimidazole derivatives have been synthesized via the aza-Michael addition reactions of1H-benzimidazoles to a,b-unsaturated compounds in water and palladium acetate obviously promoted these transformations. The reported method, overcoming the inactivation of palladium under the equivalent nitrogenous conditions, has the advantages of convenient manipulation, atom-economy, as well as environmental friendliness. The bioactive results showed that butyl 3-(5,6-dimethyl-1Hbenzo[d]imidazol-1-yl)propanoate(3c) exhibited excellent inhibitory activity against Bacillus subtilis(MIC = 16 mg/m L) and Bacillus proteus(MIC = 8 mg/m L). Therefore, this process would facilitate the construction of various potential bioactive compounds based on the benzimidazole scaffold under mild conditions.
基金financial supported by Shandong Provincial Natural Science Foundation (No. ZR2015BL009)The Key Research and Development Program of Shandong Provincial (No. 2016GGX107006)+1 种基金National Natural Science Foundation of China (No. 21501066)the Opening Project of Shanghai Key Laboratory of Chemical Biology
文摘A series of novel bridged-neonicotinoid analogues were designed and synthesized, which were constructed by starting material 8 with cyclopentenone or cyclohexenone in the presence of catalyst aluminium chloride. All of the compounds were characterized and confirmed by^1H NMR,^(13)C NMR, HRMS and IR. The bioassay tests showed that compounds 5 and 6a showed higher bioactivities than imidacloprid against Aphis craccivora.