We examined a total of 16 children with epileptic encephalopathy using fluorine-18-fluoro-2-deoxy-D-glucose （18F-FDG） positron emission computed tomography （PET）, magnetic resonance imaging （MRI） and electroence...We examined a total of 16 children with epileptic encephalopathy using fluorine-18-fluoro-2-deoxy-D-glucose （18F-FDG） positron emission computed tomography （PET）, magnetic resonance imaging （MRI） and electroencephalography. Children with infantile spasms showed significant mental retardation, severely abnormal electroencephalogram recordings, and bilateral diffuse cerebral cortex hypometabolism with I^F-FDG PET imaging. MRI in these cases showed brain atrophy, multi-micropolygyria, macrogyria, and porencephalia. In cases with Lennox-Gastaut syndrome, 18F-FDG PET showed bilateral diffuse glucose hypometabolism, while MRI showed cortical atrophy, heterotopic gray matter and tuberous sclerosis. MRI in cases with myoclonic encephalopathy demonstrated bilateral frontal and temporal cortical and white matter atrophy and 18F-FDG PET imaging showed bilateral frontal lobe atrophy with reduced bilateral frontal cortex, occipital cortex, temporal cortex and cerebellar glucose uptake. In children who could not be clearly classified, MRI demonstrated cerebral cortical atrophy and ~aF-FDG PET exhibited multifocal glucose hypometabolism. Overall, this study demonstrated that the degree of brain metabolic abnormality was consistent with clinical seizure severity. In addition, ~SF-FDG PET imaging after treatment was consistent with clinical outcomes. These findings indicate that ~SF-FDG PET can be used to assess the severity of brain injury and prognosis in children with epileptic encephalopathy.展开更多
A rapid and simple method is presented for determining β-N-oxalyl-α. β- diaminopropionic acid (β -ODAP) and its much less toxic α -isomer (α -ODAP) in Lathyrus sativus. Seed and foliage extracts of Lathyrus sat...A rapid and simple method is presented for determining β-N-oxalyl-α. β- diaminopropionic acid (β -ODAP) and its much less toxic α -isomer (α -ODAP) in Lathyrus sativus. Seed and foliage extracts of Lathyrus sativus were treated with 1-fluoro-2,4-dinitrobenzene (FDNB) and a reversed-phase high-performance liquid chromatographic method for the separation of the derivatives in the pmol range is reported.展开更多
The title compound VII, 2-fluoro-4-methyl-3-oxo-4-aza-5α-androst-1-ene-17β-carboxylic acid methyl ester （C21H30FNO3, Mr = 363.46）, was prepared through a seven-step reaction from pregnenolone, and characterized by...The title compound VII, 2-fluoro-4-methyl-3-oxo-4-aza-5α-androst-1-ene-17β-carboxylic acid methyl ester （C21H30FNO3, Mr = 363.46）, was prepared through a seven-step reaction from pregnenolone, and characterized by elemental and single-crystal X-ray diffraction analyses as well as IR, MS and 1H-NMR spectra. It is of monoclinic system, space group P21/c with a = 6.3882（7）, b = 9.9033（11）, c = 15.4925（17） , β = 91.923（2）°, V = 979.57（19） 3, Z = 2, Dc = 1.232 mg/m3, μ = 0.088 mm-1, F（000）= 392, R = 0.0465, wR = 0.0989 and λ（MoKα） = 0.71073 . The structure indicates that the four cycles （A： C（1）–C（2）–C（3）–N（1）–C（5）–C（10）, B： C（5）–C（6）–C（7）– C（8）–C（9）–C（10）, C： C（8）–C（14）–C（13）–C（12）–C（11）–C（9）, D： C（14）–C（15）–C（16）–C（17）–C（13）） are in chairand trans-configurations. The results of crystal structure determination show that there exist weak intra-molecular hydrogen bonds, resulting in a two-dimensional supramolecular frame-work of the title compound.展开更多
A novel interpenetrating structure [（HMA^＋）（FB^- ）] ·2H2O of melamine（MA） with 4-fluoro-benzoic acid （HFB） was synthesized. It crystallized in the monoclinic system with space group P21/c. The complex ha...A novel interpenetrating structure [（HMA^＋）（FB^- ）] ·2H2O of melamine（MA） with 4-fluoro-benzoic acid （HFB） was synthesized. It crystallized in the monoclinic system with space group P21/c. The complex has a interpenetrating 2D structure with hydrogen-bonded grid networks. Carboxylic acid to melamine proton transfer occurs in the complex. The adjacent HMA^＋ cations related by an inverse center form cationic [HMA^＋]∞ ribbons via a pair of N-H…N hydrogen bonds. Adjacent FB-anions are paired by C-H…F hydrogen bonds to form dimers, which are connected to [HMA^＋]∞ ribbons through N-H…O interactions. The supramolecular features in the complex are guided by control of strong N-H…N, N-H…O and O-H…O hydrogen bonds, as well as highly directional weak C-H…F interactions and aromatic π-π stacking interactions.展开更多
Fluoro-ruby was injected into the posterior funiculus of the spinal cord in the cervical （C5-T2） and lumbar （L3-6） segments of adult guinea pigs. The spinal cord was cut into serial frozen sections. The Fluoro-rub...Fluoro-ruby was injected into the posterior funiculus of the spinal cord in the cervical （C5-T2） and lumbar （L3-6） segments of adult guinea pigs. The spinal cord was cut into serial frozen sections. The Fluoro-ruby labeling was clearly delineated from the surrounding structure. The labeling traversed the cervical, thoracic and lumbar segments, and was located on the ventral portion of the posterior funiculus on the injected side, proximal to the intermediate zone of the dorsal gray matter. The fluorescence area narrowed rostro-caudally. The spinal cord, spinal cord gray matter and corticospinal tract were reconstructed using 3D-DOCTOR 4.0 software, resulting in a robust three-dimensional profile. Using functionality provided by the reconstruction software, free multi-angle observation and sectioning could be conducted on the spinal cord and corticospinal tract. Our experimental findings indicate that the Fluoro-ruby retrograde fluorescent tracing technique can accurately display the anatomical location of corticospinal tract in the guinea pig and that three-dimensional reconstruction software can be used to provide a three-dimensional image of the corticospinal tract.展开更多
A novel and simple procedure for synthesis of azanucleoside by Mitsunobu reaction between N-（p-nitrobenzyloxycarbonyl）- trans-4-hydroxy-D-proline methyl ester obtained from trans-4-hydroxy-L-proline after six-step r...A novel and simple procedure for synthesis of azanucleoside by Mitsunobu reaction between N-（p-nitrobenzyloxycarbonyl）- trans-4-hydroxy-D-proline methyl ester obtained from trans-4-hydroxy-L-proline after six-step reaction and 2-fluoro-6-azidopurine is described, and azanucleoside is fluorinated by new fluridizer 2,2-difluoro-1,3-dimethylimidazolidine （DFI）. All reactions could be carried out under mild condition.展开更多
Two Schiff base complexes [Cu（L）2] （1） and [Zn（L）2]·3H2O（2） of （E）-4-fluoro-2-（（3-morpholino propylimino）methyl）phenol （HL） have been synthesized and characterized by elemental analysis and single...Two Schiff base complexes [Cu（L）2] （1） and [Zn（L）2]·3H2O（2） of （E）-4-fluoro-2-（（3-morpholino propylimino）methyl）phenol （HL） have been synthesized and characterized by elemental analysis and single-crystal X-ray diffraction. Crystal data for 1： triclinic, space group Pī with a=4.8000（10）, b=11.109（2）, c=13.921（3）,α=66.55（3）,β=80.35（3）,γ=81.09（3）°, V=668.2（2）3 , Z=1, Dc=1.477g/cm 3 , F（000）=311, and the final R=0.0744 and wR=0.1601 for 2301 observed reflections with I 〉 2σ（I）. And those for 2： monoclinic, space group P21 /c with a=14.789（3）, b=11.713（2）, c=18.846（4）,β=107.85（3）°, V=3107.4（11）3 , Z=4, D c=1.389 g/cm 3 , F（000）=1368, and the final R=0.0749 and wR=0.1348 for 5423 observed reflections with I 〉 2σ（I）. Both 1 and 2 are four-coordinated complexes, with a square-planar geometry of copper（Ⅱ） in 1 and a slightly distorted tetrahedral geometry of zinc（Ⅱ） in 2. An asymmetric unit consists of only one half of a Cu ion and one L ligand in 1, while an asymmetric unit is composed of one Zn ion, two L ligands and three water molecules in 2. Non-classical C-H···O and C-H F hydrogen bonds play important roles in the formation of a 1D chain of 1, but O-H O and O-H N hydrogen bonds play dominant roles in the self-assembly of a 3D network of 2. The antibacterial activities of 1 and 2 against B. subtilis, S. aureus, S. faecalis, P. aeruginosa, E. coli and E. cloacae have been evaluated by MTT method.展开更多
Lithium aluminium amide [LiAI（NHR）4] 5 obtained by treating the primary amine 4 with LiAlH4 could promote the ring opening of epoxide 2 and led to high regioselective product of racemic bis[2-（6-fluoro-2-chromanyl...Lithium aluminium amide [LiAI（NHR）4] 5 obtained by treating the primary amine 4 with LiAlH4 could promote the ring opening of epoxide 2 and led to high regioselective product of racemic bis[2-（6-fluoro-2-chromanyl）-2-hydroxyethyl]amine methanesulfonic acid salt 7.展开更多
AIM:To assess the prognostic value and risk classification improvement of metabolic staging(MS)with Initial2-[18F]-fluoro-2-desoxy-D-glucose positron emission tomography(FDG-PET)in initial staging of Hodgkin’s Lympho...AIM:To assess the prognostic value and risk classification improvement of metabolic staging(MS)with Initial2-[18F]-fluoro-2-desoxy-D-glucose positron emission tomography(FDG-PET)in initial staging of Hodgkin’s Lymphoma(HL)patients to predict 5 years overall survival(5y-OS)and event free survival(EFS).METHODS:A total of 275 patients were included in this retrospective study,155 patients were staged with conventional anatomical staging(AS),and 120 also submitted to MS(FDG-PET).Prognostic analysis compared 5y-OS and 5y-EFS of patients staged with AS and MS.Risk-adjusted models incorporated clinical risk factors,computed tomography and FDG-PET staging.RESULTS:During the follow up of 267 evaluated patients,220(122 AS and 98 MS)achieved complete remission after first-line therapy(median follow-up:70±29 mo),treatment failure occurred in 79 patients and 34 died.The 5y-EFS for early vs advanced disease in AS patients was 79.3%and 66.7%,and 85.6%and53.6%in MS patients,respectively(P<0.01).The5y-OS for early and advanced disease with AS was91.3%and 81.5%,and 97.5%and 80.7%for patients staged with MS,respectively.Cox proportional hazards analysis demonstrated that FDG-PET added signifcant prognostic information and improved risk prediction(P=0.02).CONCLUSION:Initial staging FDG-PET could be used as an accurate and independent predictor of OS and EFS in HL,with impact in 5y-EFS and OS.展开更多
A series of 6-fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]quinoline-2-carboxamide derivatives was designed based on the bioisosterism and combination principle in drug design. The target compounds were synthesized fr...A series of 6-fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]quinoline-2-carboxamide derivatives was designed based on the bioisosterism and combination principle in drug design. The target compounds were synthesized from substituted aniline through Michael addition, cyclization, Mannich reaction and condensation with 4-substituted semicarbazides, and the structures were confirmed by mass spectrometry（MS） and 1H NMR. The antifungal assay was carried out in vitro by two-fold dilution. The result shows that all the compounds are of antifungal activities against the tested fungi at different levels.展开更多
Dimethylaminophenyl)-5-fluoro-6-(morpholin-4-yl)-1H-benzimidazole(1) has been synthesized and characterized by H-NMR, MS and elemental analysis. UV-Vis spectra of the 1 aqueous solutions at different pH values reveal ...Dimethylaminophenyl)-5-fluoro-6-(morpholin-4-yl)-1H-benzimidazole(1) has been synthesized and characterized by H-NMR, MS and elemental analysis. UV-Vis spectra of the 1 aqueous solutions at different pH values reveal that compound 1 can combine three protons. Its three protonation constants are determined by spectrophotometry and calculated by non-linear least squares. The results of steady-state fluorescence measurements indicate that a special interaction occurs between compound 1 and calf thymus DNA, of which the binding constant, Kb, is (2.30 ± 0.10)×l04 L/mol. Compound 1 in the concentration range of 10-8 to 1.2×10-6 mol/L could be used for quantitative determination of DNA.展开更多
基金the National Natural Science Foundation of China, No. 81071046the Guangdong Provincial Science and Technology Program, No. 2009B030801250+1 种基金2010 Guangdong Provincial Science and Technology Program, No. 2010B031600159the Guangdong Province Natural Science Foundation, No. 7001205
文摘We examined a total of 16 children with epileptic encephalopathy using fluorine-18-fluoro-2-deoxy-D-glucose （18F-FDG） positron emission computed tomography （PET）, magnetic resonance imaging （MRI） and electroencephalography. Children with infantile spasms showed significant mental retardation, severely abnormal electroencephalogram recordings, and bilateral diffuse cerebral cortex hypometabolism with I^F-FDG PET imaging. MRI in these cases showed brain atrophy, multi-micropolygyria, macrogyria, and porencephalia. In cases with Lennox-Gastaut syndrome, 18F-FDG PET showed bilateral diffuse glucose hypometabolism, while MRI showed cortical atrophy, heterotopic gray matter and tuberous sclerosis. MRI in cases with myoclonic encephalopathy demonstrated bilateral frontal and temporal cortical and white matter atrophy and 18F-FDG PET imaging showed bilateral frontal lobe atrophy with reduced bilateral frontal cortex, occipital cortex, temporal cortex and cerebellar glucose uptake. In children who could not be clearly classified, MRI demonstrated cerebral cortical atrophy and ~aF-FDG PET exhibited multifocal glucose hypometabolism. Overall, this study demonstrated that the degree of brain metabolic abnormality was consistent with clinical seizure severity. In addition, ~SF-FDG PET imaging after treatment was consistent with clinical outcomes. These findings indicate that ~SF-FDG PET can be used to assess the severity of brain injury and prognosis in children with epileptic encephalopathy.
基金Tshe prOject!(39770469) supported by the National Natural Science Foundation of China.
文摘A rapid and simple method is presented for determining β-N-oxalyl-α. β- diaminopropionic acid (β -ODAP) and its much less toxic α -isomer (α -ODAP) in Lathyrus sativus. Seed and foliage extracts of Lathyrus sativus were treated with 1-fluoro-2,4-dinitrobenzene (FDNB) and a reversed-phase high-performance liquid chromatographic method for the separation of the derivatives in the pmol range is reported.
基金supported by Young Science Fund of Key Laboratory of Advanced Textile Materials and Manufacturing Technology (Zhejiang Sci-Tech. University),Ministry of Education
文摘The title compound VII, 2-fluoro-4-methyl-3-oxo-4-aza-5α-androst-1-ene-17β-carboxylic acid methyl ester （C21H30FNO3, Mr = 363.46）, was prepared through a seven-step reaction from pregnenolone, and characterized by elemental and single-crystal X-ray diffraction analyses as well as IR, MS and 1H-NMR spectra. It is of monoclinic system, space group P21/c with a = 6.3882（7）, b = 9.9033（11）, c = 15.4925（17） , β = 91.923（2）°, V = 979.57（19） 3, Z = 2, Dc = 1.232 mg/m3, μ = 0.088 mm-1, F（000）= 392, R = 0.0465, wR = 0.0989 and λ（MoKα） = 0.71073 . The structure indicates that the four cycles （A： C（1）–C（2）–C（3）–N（1）–C（5）–C（10）, B： C（5）–C（6）–C（7）– C（8）–C（9）–C（10）, C： C（8）–C（14）–C（13）–C（12）–C（11）–C（9）, D： C（14）–C（15）–C（16）–C（17）–C（13）） are in chairand trans-configurations. The results of crystal structure determination show that there exist weak intra-molecular hydrogen bonds, resulting in a two-dimensional supramolecular frame-work of the title compound.
基金Supported by the National Natural Science Foundation of China(No.20972178)a Grant for Key Research Items in Na-tural Science of Guangdong Higher Education Institutions of China(No.06Z027)
文摘A novel interpenetrating structure [（HMA^＋）（FB^- ）] ·2H2O of melamine（MA） with 4-fluoro-benzoic acid （HFB） was synthesized. It crystallized in the monoclinic system with space group P21/c. The complex has a interpenetrating 2D structure with hydrogen-bonded grid networks. Carboxylic acid to melamine proton transfer occurs in the complex. The adjacent HMA^＋ cations related by an inverse center form cationic [HMA^＋]∞ ribbons via a pair of N-H…N hydrogen bonds. Adjacent FB-anions are paired by C-H…F hydrogen bonds to form dimers, which are connected to [HMA^＋]∞ ribbons through N-H…O interactions. The supramolecular features in the complex are guided by control of strong N-H…N, N-H…O and O-H…O hydrogen bonds, as well as highly directional weak C-H…F interactions and aromatic π-π stacking interactions.
基金supported by a grant from the Priority Academic Program Development of Jiangsu Higher Education Institutions
文摘Fluoro-ruby was injected into the posterior funiculus of the spinal cord in the cervical （C5-T2） and lumbar （L3-6） segments of adult guinea pigs. The spinal cord was cut into serial frozen sections. The Fluoro-ruby labeling was clearly delineated from the surrounding structure. The labeling traversed the cervical, thoracic and lumbar segments, and was located on the ventral portion of the posterior funiculus on the injected side, proximal to the intermediate zone of the dorsal gray matter. The fluorescence area narrowed rostro-caudally. The spinal cord, spinal cord gray matter and corticospinal tract were reconstructed using 3D-DOCTOR 4.0 software, resulting in a robust three-dimensional profile. Using functionality provided by the reconstruction software, free multi-angle observation and sectioning could be conducted on the spinal cord and corticospinal tract. Our experimental findings indicate that the Fluoro-ruby retrograde fluorescent tracing technique can accurately display the anatomical location of corticospinal tract in the guinea pig and that three-dimensional reconstruction software can be used to provide a three-dimensional image of the corticospinal tract.
文摘A novel and simple procedure for synthesis of azanucleoside by Mitsunobu reaction between N-（p-nitrobenzyloxycarbonyl）- trans-4-hydroxy-D-proline methyl ester obtained from trans-4-hydroxy-L-proline after six-step reaction and 2-fluoro-6-azidopurine is described, and azanucleoside is fluorinated by new fluridizer 2,2-difluoro-1,3-dimethylimidazolidine （DFI）. All reactions could be carried out under mild condition.
基金supported by the China Postdoctoral Science Foundation (No.20110491380)the Fundamental Research Funds for the Central Universities (No.ZYGX2009J085)
文摘Two Schiff base complexes [Cu（L）2] （1） and [Zn（L）2]·3H2O（2） of （E）-4-fluoro-2-（（3-morpholino propylimino）methyl）phenol （HL） have been synthesized and characterized by elemental analysis and single-crystal X-ray diffraction. Crystal data for 1： triclinic, space group Pī with a=4.8000（10）, b=11.109（2）, c=13.921（3）,α=66.55（3）,β=80.35（3）,γ=81.09（3）°, V=668.2（2）3 , Z=1, Dc=1.477g/cm 3 , F（000）=311, and the final R=0.0744 and wR=0.1601 for 2301 observed reflections with I 〉 2σ（I）. And those for 2： monoclinic, space group P21 /c with a=14.789（3）, b=11.713（2）, c=18.846（4）,β=107.85（3）°, V=3107.4（11）3 , Z=4, D c=1.389 g/cm 3 , F（000）=1368, and the final R=0.0749 and wR=0.1348 for 5423 observed reflections with I 〉 2σ（I）. Both 1 and 2 are four-coordinated complexes, with a square-planar geometry of copper（Ⅱ） in 1 and a slightly distorted tetrahedral geometry of zinc（Ⅱ） in 2. An asymmetric unit consists of only one half of a Cu ion and one L ligand in 1, while an asymmetric unit is composed of one Zn ion, two L ligands and three water molecules in 2. Non-classical C-H···O and C-H F hydrogen bonds play important roles in the formation of a 1D chain of 1, but O-H O and O-H N hydrogen bonds play dominant roles in the self-assembly of a 3D network of 2. The antibacterial activities of 1 and 2 against B. subtilis, S. aureus, S. faecalis, P. aeruginosa, E. coli and E. cloacae have been evaluated by MTT method.
基金the National 863 Program(No.2003AA323030)the National Natural Science Foundation of China(No.50272069 and No.20472090)for financial support.
文摘Lithium aluminium amide [LiAI（NHR）4] 5 obtained by treating the primary amine 4 with LiAlH4 could promote the ring opening of epoxide 2 and led to high regioselective product of racemic bis[2-（6-fluoro-2-chromanyl）-2-hydroxyethyl]amine methanesulfonic acid salt 7.
文摘AIM:To assess the prognostic value and risk classification improvement of metabolic staging(MS)with Initial2-[18F]-fluoro-2-desoxy-D-glucose positron emission tomography(FDG-PET)in initial staging of Hodgkin’s Lymphoma(HL)patients to predict 5 years overall survival(5y-OS)and event free survival(EFS).METHODS:A total of 275 patients were included in this retrospective study,155 patients were staged with conventional anatomical staging(AS),and 120 also submitted to MS(FDG-PET).Prognostic analysis compared 5y-OS and 5y-EFS of patients staged with AS and MS.Risk-adjusted models incorporated clinical risk factors,computed tomography and FDG-PET staging.RESULTS:During the follow up of 267 evaluated patients,220(122 AS and 98 MS)achieved complete remission after first-line therapy(median follow-up:70±29 mo),treatment failure occurred in 79 patients and 34 died.The 5y-EFS for early vs advanced disease in AS patients was 79.3%and 66.7%,and 85.6%and53.6%in MS patients,respectively(P<0.01).The5y-OS for early and advanced disease with AS was91.3%and 81.5%,and 97.5%and 80.7%for patients staged with MS,respectively.Cox proportional hazards analysis demonstrated that FDG-PET added signifcant prognostic information and improved risk prediction(P=0.02).CONCLUSION:Initial staging FDG-PET could be used as an accurate and independent predictor of OS and EFS in HL,with impact in 5y-EFS and OS.
基金Supported by the National Science and Technology Major Projects of China(No.2009ZX09301-012)
文摘A series of 6-fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]quinoline-2-carboxamide derivatives was designed based on the bioisosterism and combination principle in drug design. The target compounds were synthesized from substituted aniline through Michael addition, cyclization, Mannich reaction and condensation with 4-substituted semicarbazides, and the structures were confirmed by mass spectrometry（MS） and 1H NMR. The antifungal assay was carried out in vitro by two-fold dilution. The result shows that all the compounds are of antifungal activities against the tested fungi at different levels.
基金This work was financially supported by the National Natural Science Foundation of China(20171005)
文摘Dimethylaminophenyl)-5-fluoro-6-(morpholin-4-yl)-1H-benzimidazole(1) has been synthesized and characterized by H-NMR, MS and elemental analysis. UV-Vis spectra of the 1 aqueous solutions at different pH values reveal that compound 1 can combine three protons. Its three protonation constants are determined by spectrophotometry and calculated by non-linear least squares. The results of steady-state fluorescence measurements indicate that a special interaction occurs between compound 1 and calf thymus DNA, of which the binding constant, Kb, is (2.30 ± 0.10)×l04 L/mol. Compound 1 in the concentration range of 10-8 to 1.2×10-6 mol/L could be used for quantitative determination of DNA.
