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Asgari, Davoud,Aghanejad, Ayuob,Mojarrad, Javid Shahbazi Korean Chemical Society 2011 Bulletin of the Korean Chemical Society Vol.32 No.3
An improved convergent and economical method has been developed for the synthesis of erlotinib, a 4-anilinoquinazoline and an EGFR-tyrosine kinase inhibitor for treatment of non-small-cell lung cancer. The final two steps for the formation of this 4-anilinoquinazoline from suitable 2-aminobenzonitrile intermediate and 3-ethynylaniline were modified and were performed in a simple one-pot reaction. The ring-closing mechanism for the formation of erlotinib from the suitable formamidine intermediate and 3-ethynylaniline was investigated and determined to proceed via the formation of phenyl benzamidine intermediate rather than involving Dimroth rearrangement reported earlier. The new benzamidine intermediate was isolated for the first time and characterized.
Davoud Asgari,Ayuob Aghanejad,Javid Shahbazi Mojarrad 대한화학회 2011 Bulletin of the Korean Chemical Society Vol.32 No.3
An improved convergent and economical method has been developed for the synthesis of erlotinib, a 4-anilinoquinazoline and an EGFR-tyrosine kinase inhibitor for treatment of non-small-cell lung cancer. The final two steps for the formation of this 4-anilinoquinazoline from suitable 2-aminobenzonitrile intermediate and 3-ethynylaniline were modified and were performed in a simple one-pot reaction. The ring-closing mechanism for the formation of erlotinib from the suitable formamidine intermediate and 3-ethynylaniline was investigated and determined to proceed via the formation of phenyl benzamidine intermediate rather than involving Dimroth rearrangement reported earlier. The new benzamidine intermediate was isolated for the first time and characterized.
Covalent Immobilization of Trypsin on a Novel Aldehyde-Terminated PAMAM Dendrimer
Hamidi, Aliasghar,Rashidi, Mohammad R.,Asgari, Davoud,Aghanejad, Ayuob,Davaran, Soodabeh Korean Chemical Society 2012 Bulletin of the Korean Chemical Society Vol.33 No.7
Dendrimers are a novel class of nonlinear polymers and due to their extensive applications in different fields, called versatile polymers. Polyamidoamine (PAMAM) dendrimers are one of the most important dendrimers that have many applications in nanobiotechnology and industry. Generally aldehyde terminated dendrimers are prepared by activation of amine terminated dendrimers by glutaraldehyde which has two problems, toxicity and possibility of crosslink formation. In this study, novel aldehyde-terminated PAMAM dendrimer was prepared and used for covalent immobilization of trypsin by the aim of finding a special reagent which can prevent crosslinking and deactivation of the enzyme. For this purpose aminoacetaldehydedimethylacetal (AADA) was used as spacer group between aldehyde-terminated PAMAM and trypsin.The findings of this study showed that immobilization of trypsin not only resulted higher optimal temperature, but also increased the thermal stability of the immobilized enzyme in comparison to the free enzyme.
Preparation and Evaluation of 68Ga-ECC as a PET Renal Imaging Agent
Alireza Mirzaei,Amir Reza Jalilian,Ayuob Aghanejad,Mohammad Mazidi,Hassan Yousefnia,Gholamali Shabani,Khosro Ardaneh,Parham Geramifar,Davood Beiki 대한핵의학회 2015 핵의학 분자영상 Vol.49 No.3
Purpose Development of a gallium-68-labeled renal tracer can be a good substitute for Tc-99m, a known SPECT tracer. In this study, effort was made to develop 68Gaethylenecysteamine cysteine (68Ga-ECC). Methods Ga-ECC was prepared using generator-based 68GaCl3 and ethylenecysteamine cysteine (ECC) at optimized conditions. Stability of the complex was checked in human serum followed by partition coefficient determination of the tracer. The biodistribution of the tracer in rats was studied using tissue counting and PET/CT imaging up to 120 min. Results Ga-ECC was prepared at optimized conditions in 15 min at 90 °C (radiochemical purity ≈97±0.88 % ITLC, >99 % HPLC, specific activity: 210±5 GBq/mM). 68Ga- ECC was a water-soluble complex based on partition coefficient data (log P; −1.378) and was stable in the presence of human serum for 2 h at 37 °C. The biodistribution of the tracer demonstrated high kidney excretion of the tracer in 10– 20 min. The SUVmax ratios of the liver to left kidney were 0.38 and 0.39 for 30 and 90 min, respectively, indicating high kidney uptake. Conclusion Initial biodistribution results showed significant kidney and urinary excretion of the tracer comparable to that of the homologous 99mTc compound. The complex could be a possible PET kidney imaging agent with a fast imaging time.
Covalent Immobilization of Trypsin on a Novel Aldehyde-Terminated PAMAM Dendrimer
Aliasghar Hamidi,Mohammad R. Rashidi,Davoud Asgari,Ayuob Aghanejad,Soodabeh Davaran 대한화학회 2012 Bulletin of the Korean Chemical Society Vol.33 No.7
Dendrimers are a novel class of nonlinear polymers and due to their extensive applications in different fields, called versatile polymers. Polyamidoamine (PAMAM) dendrimers are one of the most important dendrimers that have many applications in nanobiotechnology and industry. Generally aldehyde terminated dendrimers are prepared by activation of amine terminated dendrimers by glutaraldehyde which has two problems, toxicity and possibility of crosslink formation. In this study, novel aldehyde-terminated PAMAM dendrimer was prepared and used for covalent immobilization of trypsin by the aim of finding a special reagent which can prevent crosslinking and deactivation of the enzyme. For this purpose aminoacetaldehydedimethylacetal (AADA) was used as spacer group between aldehyde-terminated PAMAM and trypsin.The findings of this study showed that immobilization of trypsin not only resulted higher optimal temperature, but also increased the thermal stability of the immobilized enzyme in comparison to the free enzyme.