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The title compound tianagliflozin triacetate 1 was synthesized and its crystal structure was determined by single-crystal X-ray diffraction.The crystal belongs to monoclinic system(C27H31ClO8,Mr = 518.97),space group P21 with a = 5.3913(11),b = 16.137(2),c = 15.411(3) ,β = 94.15(3)°,V = 1337.3(5) 3,Z = 2,Dc = 1.289 g/cm3,F(000) = 548,μ = 0.190 mm-1,the final R = 0.0374 and wR = 0.0809 for 3981 observed reflections(I 2σ(I)).The structure of 1,triacetate of a highly potent SGLT2 inhibitor tianagliflozin,was unambiguously determined by single-crystal X-ray diffraction,which helped to confirm the desired β configuration at the anomeric center and the position where the deoxylation occurred.The two benzene rings in the lattice are basically orthogonal to each other.There are four intermolecular hydrogen bonds in the crystal,which helps to further stabilize the crystal. 相似文献
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王玉丽胡海平 《应用数学与计算数学学报》2018,(3):572-580
提出用概率协同表示(probabilistic collaborative representation-based classifier, ProCRC)的方法生成权重系数对所提取的动作特征进行更新.首先,利用深度学习的思想将人体不同动作的视频分为5层;然后分别对各层的节点进行特征提取,同时,运用ProCRC产生梯度下降法所需的权重向量,对所提取的特征进行更新;最后,基于张量的思想进行特征的聚类分析.仿真实验结果表明,该方法优于稀疏表示的方法(sparse representation-based classifier, SRC). 相似文献
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含噻唑环的二肽基肽酶IV抑制剂的设计、合成和降血糖活性研究 总被引:1,自引:0,他引:1
设计并合成了16个含噻唑环的二肽基肽酶IV (DPP-IV)抑制剂, 利用IR, 1H NMR, 13C NMR和HR-MS表征了它们的结构. 通过小鼠口服糖耐量实验测试了它们的降血糖作用, 结果显示其中两个化合物具有很强的降血糖作用, 一个与格列齐特相当, 另一个强于格列齐特, 显示了在治疗II型糖尿病方面的前景. 构效关系研究发现, 这16个化合物的构效关系呈现出明显的规律. 相似文献
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The title compound was synthesized and its crystal structure was determined by single-crystal X-ray diffraction.The crystal is of monoclinic system(C31H37ClO10,Mr = 605.06),space group P21 with a = 11.882(5),b = 10.106(5),c = 13.816(6),V = 1545.9(12)3,Z = 2,Dc = 1.300 g/cm3,F(000) = 640,μ = 0.179 mm-1,the final R = 0.0430 and wR = 0.0595 for 4960 observed reflections(I > 2σ(I)).The title compound was confirmed to be a β-anomer by single-crystal X-ray diffraction and 1H NMR.The proximal benzene ring is nearly orthogonal to the glucopyranoside ring,and the two benzene rings are also almost orthogonal to each other.Four non-classical intermolecular hydrogen bonds observed in the crystal lattice help to stabilize the crystal. 相似文献
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以Canagliflozin(1)为起始原料,经7步反应合成了其6-OH脱氧产物4-(6-脱氧-β-D-吡喃葡萄糖基)-2-[5-(4-氟苯基)噻吩-2-甲基]-1-甲基苯(8),8是与母体1相似的新型SGLT2抑制剂,总收率21%,其结构经1H NMR,13C NMR和MS表征。体外生物活性测试结果显示,1和8对hSGLT2的IC50分别为3.9 nM和4.8nM,对SGLT1的选择性(SGLT2/SGLT1)分别为178和194。在大鼠尿糖排泄实验(UGE)中8具有很强的尿糖排泄作用,与母体1并无显著性差异。 相似文献