Two series of novel derivatives of4,5,6,7-tetrahydrothieno [3,2-c]pyridine were synthesized and structurally characterized by 1^H NMR and MS. Their in vivo antiplatelet aggregation activities were evaluated.
A series of novel derivatives of 4, 5, 6, 7-tetrahydrothieno [3,2-c] pyridine were synthesized and structurally characterized by 1H NMR and MS. Their in vivo anti-platelet aggregation activities were evaluated. A 3D-Q...A series of novel derivatives of 4, 5, 6, 7-tetrahydrothieno [3,2-c] pyridine were synthesized and structurally characterized by 1H NMR and MS. Their in vivo anti-platelet aggregation activities were evaluated. A 3D-QSAR was performed using the CoMFA and the CoMSIA. This model provided useful guidelines for novel anti-platelet thienopyridines design.展开更多
By means of 'Mortar Bar Method',the ratio of cement to aggregate was kept as a constant 1∶2.25,the water cement ratio of the mixture was 0.40,and six prism specimens were prepared for each batch of mixing pr...By means of 'Mortar Bar Method',the ratio of cement to aggregate was kept as a constant 1∶2.25,the water cement ratio of the mixture was 0.40,and six prism specimens were prepared for each batch of mixing proportions with dimensions of 10×10×60mm 3 at 38±2℃ and RH≥95%, the influences of content and particle size of active aggregate, sort and content of alkali component and type of slag on the expansion ratios of alkali activated slag cement(ASC) mortars due to alkali aggregate reaction(AAR) were studied. According to atomic absorption spectrometry,the amount of free alkali was measured in ASC mortars at 90d.The results show above factors affect AAR remarkably,but no dangerous AAR will occur in ASC system when the amount of active aggregate is below 15% and the mass fraction of alkali is not more than 5% (Na 2O).Alkali participated in reaction as an independent component, and some hydrates containing alkali cations were produced, free alkalis in ASC system can be reduced enormously.Moreover,slag is an effective inhibitor, the possibility of generating dangerous AAR in ASC system is much lower at same conditions than that in ordinary Portland cement system.展开更多
Biotransformation ofα-asarone by Alternaria longipes CGMCC 3.2875 yielded two pairs of new neolignans,(+)(7 S,8 S,7’S,8’R)iso-magnosalicin(1 a)/(-)(7 R,8 R,7’R,8’S)iso-magnosalicin(1 b)and(+)(7 R,8 R,7’S,8’R)ma...Biotransformation ofα-asarone by Alternaria longipes CGMCC 3.2875 yielded two pairs of new neolignans,(+)(7 S,8 S,7’S,8’R)iso-magnosalicin(1 a)/(-)(7 R,8 R,7’R,8’S)iso-magnosalicin(1 b)and(+)(7 R,8 R,7’S,8’R)magnosalicin(2 a)/(-)(7 S,8 S,7’R,8’S)magnosalicin(2 b),and four known metabolites,(±)acoraminol A(3),(±)acoraminol B(4),asaraldehyde(5),and 2,4,5-trimethoxybenzoic acid(6).Their structures,including absolute configurations,were determined by extensive analysis of NMR spectra,X-ray crystallography,and quantum chemical ECD calculations.The cytotoxic activity and Aβ_(42)aggregation inhibitory activity of all the compounds were evaluated.Compound 2 displayed significant anti-Aβ_(42)aggregation activity with an inhibitory rate of 60.81%(the positive control EGCG:69.17%).In addition the biotransformation pathway ofα-asarone by Alternaria longipes CGMCC 3.2875 was proposed.展开更多
文摘Two series of novel derivatives of4,5,6,7-tetrahydrothieno [3,2-c]pyridine were synthesized and structurally characterized by 1^H NMR and MS. Their in vivo antiplatelet aggregation activities were evaluated.
文摘A series of novel derivatives of 4, 5, 6, 7-tetrahydrothieno [3,2-c] pyridine were synthesized and structurally characterized by 1H NMR and MS. Their in vivo anti-platelet aggregation activities were evaluated. A 3D-QSAR was performed using the CoMFA and the CoMSIA. This model provided useful guidelines for novel anti-platelet thienopyridines design.
文摘By means of 'Mortar Bar Method',the ratio of cement to aggregate was kept as a constant 1∶2.25,the water cement ratio of the mixture was 0.40,and six prism specimens were prepared for each batch of mixing proportions with dimensions of 10×10×60mm 3 at 38±2℃ and RH≥95%, the influences of content and particle size of active aggregate, sort and content of alkali component and type of slag on the expansion ratios of alkali activated slag cement(ASC) mortars due to alkali aggregate reaction(AAR) were studied. According to atomic absorption spectrometry,the amount of free alkali was measured in ASC mortars at 90d.The results show above factors affect AAR remarkably,but no dangerous AAR will occur in ASC system when the amount of active aggregate is below 15% and the mass fraction of alkali is not more than 5% (Na 2O).Alkali participated in reaction as an independent component, and some hydrates containing alkali cations were produced, free alkalis in ASC system can be reduced enormously.Moreover,slag is an effective inhibitor, the possibility of generating dangerous AAR in ASC system is much lower at same conditions than that in ordinary Portland cement system.
基金supported by the National Key Research and Development Program of China(Nos.2018YFA0903200 and 2018YFA0903201)the National Natural Science Foundation of China(Nos.81925037 and 31900284)+3 种基金the Chang Jiang Scholars Program(Young Scholar)from the Ministry of Education of China(GAO Hao,2017)the National High-level Personnel of Special Support Program(No.2017RA2259)the Local Innovative and Research Teams Project of Guangdong Pearl River Talents Program(No.2017BT01Y036)K.C.Wong Education Foundation(GAO Hao,2016)。
文摘Biotransformation ofα-asarone by Alternaria longipes CGMCC 3.2875 yielded two pairs of new neolignans,(+)(7 S,8 S,7’S,8’R)iso-magnosalicin(1 a)/(-)(7 R,8 R,7’R,8’S)iso-magnosalicin(1 b)and(+)(7 R,8 R,7’S,8’R)magnosalicin(2 a)/(-)(7 S,8 S,7’R,8’S)magnosalicin(2 b),and four known metabolites,(±)acoraminol A(3),(±)acoraminol B(4),asaraldehyde(5),and 2,4,5-trimethoxybenzoic acid(6).Their structures,including absolute configurations,were determined by extensive analysis of NMR spectra,X-ray crystallography,and quantum chemical ECD calculations.The cytotoxic activity and Aβ_(42)aggregation inhibitory activity of all the compounds were evaluated.Compound 2 displayed significant anti-Aβ_(42)aggregation activity with an inhibitory rate of 60.81%(the positive control EGCG:69.17%).In addition the biotransformation pathway ofα-asarone by Alternaria longipes CGMCC 3.2875 was proposed.
