Indole[2,1-α]isoquinolines are an important class of bioactive molecules and show good antibacterial activity.In the present study,an efficient copper(I)-catalyzed acylation/cyclization has been developed for the con...Indole[2,1-α]isoquinolines are an important class of bioactive molecules and show good antibacterial activity.In the present study,an efficient copper(I)-catalyzed acylation/cyclization has been developed for the construction of indolo[2,1-α]isoquinoline derivatives by utilizing 2-aryl-N-acryloyl indole and benzohydrazide as reactants in the presence of CuI as catalyst and tert-butyl hydroperoxide as oxidant.The present protocol exhibits good functional group tolerance,and a series of acylated indole[2,1-α]isoquinolines were synthesized in moderate to good yields.Radical trapping experiments indicated that the reaction may involve a radical process.展开更多
A series of benzohydrazide derivatives as novel ribosomal S6 kinase 2 （RSK2） inhibitors were designed and synthesized from a hit compound previously discovered by ligand-based virtual screening. Biological assays sh...A series of benzohydrazide derivatives as novel ribosomal S6 kinase 2 （RSK2） inhibitors were designed and synthesized from a hit compound previously discovered by ligand-based virtual screening. Biological assays showed that these compounds possessed moderate inhibitory activities towards RSK2. The structural activity relationships （SAR） were elucidated by molecular docking and further optimization was performed.展开更多
A novel 4-tert-butyl-N’-(4-(1,2,2-triphenylvinyl)benzylidene)benzohydrazide(TBB)was successfully synthesized in simple one-step process.It was characterized by FT-IR,1H NMR,13C NMR and HRMS.Its fluorescence sensing a...A novel 4-tert-butyl-N’-(4-(1,2,2-triphenylvinyl)benzylidene)benzohydrazide(TBB)was successfully synthesized in simple one-step process.It was characterized by FT-IR,1H NMR,13C NMR and HRMS.Its fluorescence sensing ability to 15 metal ions was investigated.Weak emission from TBB could be efficiently increased by trace Hg^2+,through coordination reaction between TBB and Hg^2+ with"turn on"character.The fluorescence intensity of TBB/Hg^2+([TBB]=3.0×10^–6 mol/L,[Hg2+]=1.3×10^–4 mol/L)was 7.5 times higher than that of TBB.This TBB sensor exhibited high selectivity for Hg^2+ and other metal ions did not interfere in this determination.The limit of detection was 0.566μmol/L(S/N=3).The experimental results showed that this TBB sensor could sensitively respond to Hg^2+ within concentration range(from 5×10–6 mol/L to 1.3×10^–4 mol/L).展开更多
The one-pot four-component reaction of benzohydrazide,acetylenedicarboxylate,aromatic aldehydes and malononitrile in ethanol with triethylamine as base catalyst afforded functionalized 1-benzamido-1,4-dihydropyridines...The one-pot four-component reaction of benzohydrazide,acetylenedicarboxylate,aromatic aldehydes and malononitrile in ethanol with triethylamine as base catalyst afforded functionalized 1-benzamido-1,4-dihydropyridines in satisfactory yields.Under similar conditions,picolinohydrazide or nicotinohydrazide can also be successfully utilized in the reactions to give corresponding functionalized 1,4-dihydropyridines.1H NMR data indicated that an equilibrium of cis/trans-conformations exist in 1-benzamido-1,4-dihydropyridines.展开更多
文摘Indole[2,1-α]isoquinolines are an important class of bioactive molecules and show good antibacterial activity.In the present study,an efficient copper(I)-catalyzed acylation/cyclization has been developed for the construction of indolo[2,1-α]isoquinoline derivatives by utilizing 2-aryl-N-acryloyl indole and benzohydrazide as reactants in the presence of CuI as catalyst and tert-butyl hydroperoxide as oxidant.The present protocol exhibits good functional group tolerance,and a series of acylated indole[2,1-α]isoquinolines were synthesized in moderate to good yields.Radical trapping experiments indicated that the reaction may involve a radical process.
基金The Fundamental Research Funds for the Central Universitiesthe National Natural Science Foundation of China(Grants No.21173076,81102375and81102420)+3 种基金the Specialized Research Fund for the Doctoral Program of Higher Education of China(Grants No.20090074120012 and 20110074120009)the Shanghai Committee of Science and Technology(Grants No.11DZ2260600 and 10431902600)the Innovation Program of Shanghai Municipal Education Commission(Grant No.10ZZ41)the 863 Hi-Tech Program of China(Grant No.2012AA020308)
文摘A series of benzohydrazide derivatives as novel ribosomal S6 kinase 2 （RSK2） inhibitors were designed and synthesized from a hit compound previously discovered by ligand-based virtual screening. Biological assays showed that these compounds possessed moderate inhibitory activities towards RSK2. The structural activity relationships （SAR） were elucidated by molecular docking and further optimization was performed.
基金Anhui Provincial Teaching Team of Organic Chemistry(2017jxtd051)2019 University Outstanding Young Talents Support Program Project(General Project)of Anhui Province(gxyq2019108)+1 种基金the Major Basic Research Project of the Natural Science Foundation of the Anhui Province Education Department(KJ2016A512)the Natural Science Foundation of Chizhou University(CZ2019ZRZ01)。
文摘A novel 4-tert-butyl-N’-(4-(1,2,2-triphenylvinyl)benzylidene)benzohydrazide(TBB)was successfully synthesized in simple one-step process.It was characterized by FT-IR,1H NMR,13C NMR and HRMS.Its fluorescence sensing ability to 15 metal ions was investigated.Weak emission from TBB could be efficiently increased by trace Hg^2+,through coordination reaction between TBB and Hg^2+ with"turn on"character.The fluorescence intensity of TBB/Hg^2+([TBB]=3.0×10^–6 mol/L,[Hg2+]=1.3×10^–4 mol/L)was 7.5 times higher than that of TBB.This TBB sensor exhibited high selectivity for Hg^2+ and other metal ions did not interfere in this determination.The limit of detection was 0.566μmol/L(S/N=3).The experimental results showed that this TBB sensor could sensitively respond to Hg^2+ within concentration range(from 5×10–6 mol/L to 1.3×10^–4 mol/L).
基金This work was financially supported by the National Natural Science Foundation of China(No.21272200)the Priority Academic Program Development of Jiangsu Higher Education Institutions.
文摘The one-pot four-component reaction of benzohydrazide,acetylenedicarboxylate,aromatic aldehydes and malononitrile in ethanol with triethylamine as base catalyst afforded functionalized 1-benzamido-1,4-dihydropyridines in satisfactory yields.Under similar conditions,picolinohydrazide or nicotinohydrazide can also be successfully utilized in the reactions to give corresponding functionalized 1,4-dihydropyridines.1H NMR data indicated that an equilibrium of cis/trans-conformations exist in 1-benzamido-1,4-dihydropyridines.
