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血管生成抑制蛋白1、血清沉默信息调节因子1、血栓素-B_(2)在2型糖尿病肾病中的水平变化及与白蛋白尿进展的关系分析 被引量:1
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作者 蒋琳 陆璧 +1 位作者 张彦 李梦婷 《陕西医学杂志》 CAS 2024年第1期46-50,共5页
目的:探究血管生成抑制蛋白1(VASH-1)、血清沉默信息调节因子1(Sirt1)与血栓素-B2(TXB2)在2型糖尿病肾病中的水平变化及与白蛋白尿进展的关系。方法:选取198例2型糖尿病肾病患者纳入研究组,另选100例无肾脏损害的2型糖尿病患者为对照组... 目的:探究血管生成抑制蛋白1(VASH-1)、血清沉默信息调节因子1(Sirt1)与血栓素-B2(TXB2)在2型糖尿病肾病中的水平变化及与白蛋白尿进展的关系。方法:选取198例2型糖尿病肾病患者纳入研究组,另选100例无肾脏损害的2型糖尿病患者为对照组,对患者进行随访,检测记录患者的血清VASH-1、Sirt1、TXB2水平,并根据患者是否发生白蛋白尿分层研究,分析VASH-1、Sirt1、TXB2水平与患者白蛋白尿进展的关系。结果:与对照组比较,研究组患者的血清VASH-1、Sirt1水平降低,TXB2水平升高(均P<0.05)。与进展组患者相比较,维持组患者的血清VASH-1、Sirt1水平升高,TXB2水平降低(均P<0.05)。进展组和维持组患者的空腹血糖(FPG)、餐后2h血糖(2hPG)、空腹胰岛素(FINS)、糖化血红蛋白(HbA1c)、胰岛素抵抗指数(HOMA-IR)水平比较差异无统计学意义(均P>0.05)。以研究组患者是否发生白蛋白尿进展为因变量,以患者的血清VASH-1、Sirt1、TXB2水平为自变量,进行多因素Logistic回归分析,可知血清VASH-1、Sirt1、TXB2水平均会对患者发生白蛋白尿进展产生影响(均P<0.05)。采用ROC曲线探究2型糖尿病肾病患者血清VASH-1、Sirt1、TXB2水平对白蛋白尿进展的预测价值,其AUC值分别为0.943、0.758、0.894(均P<0.05)。结论:2型糖尿病肾病患者的血清VASH-1和Sirt1的水平下降,TXB2的水平上升,其水平变化与白蛋白尿的进展有关,对糖尿病肾病患者发生白蛋白尿进展具有一定预测价值。 展开更多
关键词 血管生成抑制蛋白1 血清沉默信息调节因子1 血栓素-b2 2型糖尿病肾病 白蛋白尿
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基于1H-吡唑并[3,4-b]吡啶母核PI3Kδ抑制剂的设计合成
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作者 田宇奇 兰明 +1 位作者 王强 郑永胜 《洛阳理工学院学报(自然科学版)》 2024年第2期1-9,共9页
恶性肿瘤严重危害人类健康与生命,磷脂酰肌醇-3激酶家族(PI3Ks)在细胞增殖、分化过程中起着重要作用,该激酶及其相关通路的其他激酶可被药物干预,是抗癌药物的热门靶点。在以往的PI3K抑制剂中,均有1H-吡唑并[3,4-b]吡啶母核,通过虚拟筛... 恶性肿瘤严重危害人类健康与生命,磷脂酰肌醇-3激酶家族(PI3Ks)在细胞增殖、分化过程中起着重要作用,该激酶及其相关通路的其他激酶可被药物干预,是抗癌药物的热门靶点。在以往的PI3K抑制剂中,均有1H-吡唑并[3,4-b]吡啶母核,通过虚拟筛选以及合成路线设计,合成了一系列1H-吡唑并[3,4-b]吡啶类化合物,该类化合物可能对PI3Kδ具有潜在抑制作用。 展开更多
关键词 PI3K抑制剂 有机合成 1H-吡唑并[3 4-b]吡啶 抗癌药
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Pulmonary Edema and Pleural Effusion Detection Using Efficient Net-V1-B4 Architecture and AdamW Optimizer from Chest X-Rays Images
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作者 Anas AbuKaraki Tawfi Alrawashdeh +4 位作者 Sumaya Abusaleh Malek Zakarya Alksasbeh Bilal Alqudah Khalid Alemerien Hamzah Alshamaseen 《Computers, Materials & Continua》 SCIE EI 2024年第7期1055-1073,共19页
This paper presents a novelmulticlass systemdesigned to detect pleural effusion and pulmonary edema on chest Xray images,addressing the critical need for early detection in healthcare.A new comprehensive dataset was f... This paper presents a novelmulticlass systemdesigned to detect pleural effusion and pulmonary edema on chest Xray images,addressing the critical need for early detection in healthcare.A new comprehensive dataset was formed by combining 28,309 samples from the ChestX-ray14,PadChest,and CheXpert databases,with 10,287,6022,and 12,000 samples representing Pleural Effusion,Pulmonary Edema,and Normal cases,respectively.Consequently,the preprocessing step involves applying the Contrast Limited Adaptive Histogram Equalization(CLAHE)method to boost the local contrast of the X-ray samples,then resizing the images to 380×380 dimensions,followed by using the data augmentation technique.The classification task employs a deep learning model based on the EfficientNet-V1-B4 architecture and is trained using the AdamW optimizer.The proposed multiclass system achieved an accuracy(ACC)of 98.3%,recall of 98.3%,precision of 98.7%,and F1-score of 98.7%.Moreover,the robustness of the model was revealed by the Receiver Operating Characteristic(ROC)analysis,which demonstrated an Area Under the Curve(AUC)of 1.00 for edema and normal cases and 0.99 for effusion.The experimental results demonstrate the superiority of the proposedmulti-class system,which has the potential to assist clinicians in timely and accurate diagnosis,leading to improved patient outcomes.Notably,ablation-CAM visualization at the last convolutional layer portrayed further enhanced diagnostic capabilities with heat maps on X-ray images,which will aid clinicians in interpreting and localizing abnormalities more effectively. 展开更多
关键词 Image classification decision support system EfficientNet-V1-b4 AdamW optimizer pulmonary edema pleural effusion chest X-rays
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Novel miR-490-3p/hnRNPA1-b/PKM2 axis mediates the Warburg effect and proliferation of colon cancer cells via the PI3K/AKT pathway
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作者 Xiang-Hui Wan Guo-Bing Jin +8 位作者 Qun Yang Ji-Long Hu Zhi-Liang Liu Jun Rao Can Wen Peng-Ling Li Xi-Mei Yang Bo Huang Xiao-Zhong Wang 《World Journal of Gastrointestinal Oncology》 SCIE 2024年第5期2038-2059,共22页
BACKGROUND Heterogeneous ribonucleoprotein A1(hnRNPA1)has been reported to enhance the Warburg effect and promote colon cancer(CC)cell proliferation,but the role and mechanism of the miR-490-3p/hnRNPA1-b/PKM2 axis in ... BACKGROUND Heterogeneous ribonucleoprotein A1(hnRNPA1)has been reported to enhance the Warburg effect and promote colon cancer(CC)cell proliferation,but the role and mechanism of the miR-490-3p/hnRNPA1-b/PKM2 axis in CC have not yet been elucidated.AIM To investigate the role and mechanism of a novel miR-490-3p/hnRNPA1-b/PKM2 axis in enhancing the Warburg effect and promoting CC cell proliferation through the PI3K/AKT pathway.METHODS Paraffin-embedded pathological sections from 220 CC patients were collected and subjected to immunohistochemical analysis to determine the expression of hnRNPA1-b.The relationship between the expression values and the clinicopathological features of the patients was investigated.Differences in mRNA expression were analyzed using quantitative real-time polymerase chain reaction,while differences in protein expression were analyzed using western blot.Cell proliferation was evaluated using the cell counting kit-8 and 5-ethynyl-2’-deoxyuridine assays,and cell cycle and apoptosis were detected using flow cytometric assays.The targeted binding of miR-490-3p to hnRNPA1-b was validated using a dual luciferase reporter assay.The Warburg effect was evaluated by glucose uptake and lactic acid production assays.RESULTS The expression of hnRNPA1-b was significantly increased in CC tissues and cells compared to normal controls(P<0.05).Immunohistochemical results demonstrated significant variations in the expression of the hnRNPA1-b antigen in different stages of CC,including stage I,II-III,and IV.Furthermore,the clinicopathologic characterization revealed a significant correlation between hnRNPA1-b expression and clinical stage as well as T classification.HnRNPA1-b was found to enhance the Warburg effect through the PI3K/AKT pathway,thereby promoting proliferation of HCT116 and SW620 cells.However,the proliferation of HCT116 and SW620 cells was inhibited when miR-490-3p targeted and bound to hnRNPA1-b,effectively blocking the Warburg effect.CONCLUSION These findings suggest that the novel miR-490-3p/hnRNPA1-b/PKM2 axis could provide a new strategy for the diagnosis and treatment of CC. 展开更多
关键词 Heterogeneous ribonucleoprotein A1-b MiR-490-3p Colon cancer Alternative splicing Warburg effect
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西格列汀通过上调TTF-1/SP-B通路对LPS诱导小鼠急性肺损伤的保护作用 被引量:1
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作者 王小川 杜发旺 +6 位作者 姚宇 李丽 何高燕 王汉超 王勤 熊伟 朱涛 《西南医科大学学报》 2023年第6期495-499,共5页
目的 探讨小鼠急性肺损伤(acute lung injury,ALI)状态下DPP4(dipeptidyl peptidase 4 inhibitor,DPP4I)抑制剂西格列汀对肺组织的保护作用及潜在的分子机制。方法 将32只雄性BALB/C小鼠随机分为对照组、DPP4抑制剂西格列汀组(DPP4I组)... 目的 探讨小鼠急性肺损伤(acute lung injury,ALI)状态下DPP4(dipeptidyl peptidase 4 inhibitor,DPP4I)抑制剂西格列汀对肺组织的保护作用及潜在的分子机制。方法 将32只雄性BALB/C小鼠随机分为对照组、DPP4抑制剂西格列汀组(DPP4I组)、内毒素组(LPS组)和LPS+DPP4I组,每组8只。采用气道内注射LPS建立小鼠ALI模型,72 h后获取标本,通过HE染色观察肺组织病理学改变及损伤评分,采用Diff-Quik染色对肺泡灌洗液(alveolar larage fluid,BALF)中炎症细胞分类计数,使用湿/干比(W/D)检测肺水肿程度,使用qPCR和western blotting法分析肺组织中甲状腺转录因子-1(thyroid transcription Factor 1,TTF-1)和表面活性物质相关蛋白-B(surfactant-associated protein-B,SP-B)的mRNA和蛋白表达水平。结果 小鼠气道内注射LPS干预72 h后,肺组织出现明显的病理学改变,肺损伤评分增加,肺水肿指标W/D显著升高,BALF中细胞总数、中性粒细胞数、巨噬细胞数和淋巴细胞数明显增多,肺组织中TTF-1和SP-B的mRNA和蛋白表达水平明显降低,差异均有统计学意义(P <0.05)。对照组与DPP4I组未见明显病理改变。与LPS组相比,LPS+DPP4I组小鼠的肺组织病理改变程度、肺损伤评分、W/D比值、BALF中细胞总数、中性粒细胞数、巨噬细胞数和淋巴细胞数均明显更低,肺组织TTF-1和SP-B的mRNA和蛋白表达水平均明显更高(P <0.05)。结论 在小鼠ALI模型中DPP4抑制剂西格列汀可能通过上调肺组织TTF-1促进SP-B分泌,减轻肺损伤和炎症反应水平,为DPP4I应用于急性呼吸窘迫综合征(acute respiratory distress syndrome,ARDS)的临床治疗奠定了实验基础。 展开更多
关键词 急性肺损伤 DPP4抑制剂 西格列汀 甲状腺转录因子-1 表面活性物质相关蛋白-b
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芍药甘草汤对Oddi括约肌功能障碍豚鼠自噬相关蛋白Beclin1和LC3-B的影响
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作者 胡永红 陈萌 +3 位作者 王旋 陈晓东 张晞文 李甫 《辽宁中医杂志》 CAS 2023年第10期220-224,I0006,共6页
目的探讨芍药甘草汤对豚鼠Oddi括约肌功能障碍的治疗作用及其对自噬相关蛋白Beclin1和LC3-B表达的影响。方法30只豚鼠随机分为正常组、模型组和芍药甘草汤治疗组,每组10只。模型组和芍药甘草汤组按0.6 mg/kg体质量静脉注射吗啡注射液以... 目的探讨芍药甘草汤对豚鼠Oddi括约肌功能障碍的治疗作用及其对自噬相关蛋白Beclin1和LC3-B表达的影响。方法30只豚鼠随机分为正常组、模型组和芍药甘草汤治疗组,每组10只。模型组和芍药甘草汤组按0.6 mg/kg体质量静脉注射吗啡注射液以诱导Oddi括约肌功能障碍模型,正常组豚鼠予等体积0.9%氯化钠溶液静脉注射,每周三次;从第一次造模起,芍药甘草汤组按12.5 g/kg灌胃治疗;正常组和模型组分别予等体积0.4%羧甲基纤维素钠(CMC-Na)灌胃,1次/d,共计4周。末次给药后禁食,收集血清和Oddi括约肌组织。全自动生化分析仪检测血清丙氨酸氨基转移酶(ALT)、天冬氨酸氨基转移酶(AST)水平;H&E染色检测Oddi括约肌病理变化;qRT-PCR检测c-Kit、Beclin1、LC3-B mRNA表达;Western blot检测c-Kit、Beclin1、LC3-B蛋白表达。结果(1)与对照组相比,模型组豚鼠血清ALT、AST水平显著增高(P<0.01);与模型组相比,芍药甘草汤组豚鼠血清ALT、AST水平均明显下降(P<0.05)。(2)H&E染色显示,模型组豚鼠Oddi括约肌纤维排列不规则、部分紊乱,并可见炎性细胞浸润,黏膜下纤维组织增生明显、平滑肌层显著增厚;与模型组相比,芍药甘草汤组豚鼠Oddi括约肌组织中纤维排列紊乱、炎性细胞浸润及黏膜下纤维组织增生明显改善。(3)与正常组相比,模型组豚鼠Oddi括约肌中c-Kit的mRNA和蛋白表达显著降低(P<0.01,P<0.05),自噬相关Beclin1和LC3-B的mRNA和蛋白表达明显增加(P<0.01,P<0.05);与模型组相比,芍药甘草汤组c-Kit的mRNA和蛋白表达明显升高(P<0.01),Beclin1和LC3-B的mRNA和蛋白表达则显著减少(P<0.01)。结论芍药甘草汤可有效治疗吗啡诱导的豚鼠Oddi括约肌功能障碍,其作用机制可能是与减少细胞过度自噬、提升Cajal细胞活性有关。 展开更多
关键词 芍药甘草汤 ODDI括约肌功能障碍 自噬 BECLIN1 LC3-b
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Synthesis and plant-growth regulatory activities of novel imine derivatives containing 1H-1,2,4-triazole and thiazole rings 被引量:6
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作者 Qin, Xue Yu, Hai Bo +5 位作者 Dai, Hong Qin, Zhen Fang Zhang, Xin Bing, Gui Fang Wang, Ting Ting Fang, Jian Xin 《Chinese Chemical Letters》 SCIE CAS CSCD 2010年第3期283-286,共4页
Eleven new imine derivatives 6 containing 1H-1,2,4-triazole and thiazole rings were synthesized by the condensation of 5-((1H- 1,2,4-triazol-1-yl)methyl)-4-tert-butylthiazol-2-amine with various substituted benzaldehy... Eleven new imine derivatives 6 containing 1H-1,2,4-triazole and thiazole rings were synthesized by the condensation of 5-((1H- 1,2,4-triazol-1-yl)methyl)-4-tert-butylthiazol-2-amine with various substituted benzaldehydes.The structures of the title compounds were characterized by ~1H NMR,MS and elemental analysis.The plant-growth regulatory activities of these compounds were evaluated.The primary bioassay results indicated that these target compounds exhibited promising plant-growth regulatory activities. 展开更多
关键词 1H-1 2 4-Triazole thiazole SYNTHESIS IMINE Plant-growth regulatory activity
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Synthesis and Structural Characterization of a Tetranuclear Copper Complex with 2-Amino-1,3-thiazole 被引量:1
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作者 邓玉恒 丁彦峰 +1 位作者 刘娟 单晓晨 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2010年第12期1818-1823,共6页
The title tetranuclear complex,(μ4-oxo)-hexakis(μ2-chloro)-tetrakis(2-amino-1,3-thiazole-N)-tetra-copper(ii) [Cu4(μ4-O)(μ-Cl)6L4](1,L=2-amino-1,3-thiazole) was synthesized by the reaction of CuCl2... The title tetranuclear complex,(μ4-oxo)-hexakis(μ2-chloro)-tetrakis(2-amino-1,3-thiazole-N)-tetra-copper(ii) [Cu4(μ4-O)(μ-Cl)6L4](1,L=2-amino-1,3-thiazole) was synthesized by the reaction of CuCl2·2H2O with 2-amino-1,3-thiazole in methanol and characterized by IR spectra and X-ray diffraction.Complex 1 crystallizes in triclinic,space group P1 with a=9.7137(2),b=10.7005(2),c=14.6505(2),α=83.9550(10),β=82.0930(10),γ=67.1640(10)°,V=1387.84(4)3,Mr=883.43,Z=2,μ=3.927 mm-1,Dc=2.1144 g/cm3,F(000)=868,R=0.0332 and wR=0.0814.The complex contains a tetrahedron of four CuII atoms coordinating to a central μ4-O atom,with the six edges of the tetrahedron bridged by six Cl atoms.The Cu-O bond distances range from 1.910(2) to 1.918(2),Cu-Cl from 2.3501(11) to 2.5924(10),and Cu-Cu from 3.1003(6) to 3.1663(6).The coordination geometries of the four coppers distort from trigonal bipramid to tetragonal pyramid with different distortion factors.The free animo groups of the ligands result in a lot of N-H···Cl and N-H···N intra-and intermolecular hydrogen bonds. 展开更多
关键词 2-amino-1 3-thiazole TETRANUCLEAR copper complex crystal structure
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Synthesis, Crystal Structure and Antitumor Activity of (E)-4-tert-Butyl-N-(2,4-dichlorobenzylidene)-5-(1,2,4-triazol-1-yl)-thiazol-2-amine 被引量:5
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作者 胡艾希 覃智 +1 位作者 叶姣 夏曙 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2010年第11期1680-1683,共4页
The title compound (E)-4-tert-butyl-N-(2,4-dichlorobenzylidene)-5-(1,2,4-triazol-1-yl)-thiazol-2-amine was synthesized by the reaction of 4-tert-butyl-5-(1,2,4-triazol-1-yl)-thiazol-2-amine with 2,4-dichlorobe... The title compound (E)-4-tert-butyl-N-(2,4-dichlorobenzylidene)-5-(1,2,4-triazol-1-yl)-thiazol-2-amine was synthesized by the reaction of 4-tert-butyl-5-(1,2,4-triazol-1-yl)-thiazol-2-amine with 2,4-dichlorobenzaldehyde, and its crystal structure was determined by singlecrystal X-ray diffraction. The crystal belongs to the triclinic system, space group P1 with a = 7.9748(4), b = 10.1803(5), c = 11.4603(6), α = 102.882(1), β = 100.253(1), γ = 104.457(1)°, V = 850.95(7)3, Z = 2, F(000) = 392, C16H15Cl2N5S, Mr = 380.29, Dc = 1.484 g/cm3, S = 1.095, μ = 0.512 mm-1, the final R = 0.0301 and wR = 0.0965 for 3334 observed reflections (I 〉 2σ(I)). The preliminary antitumor activity shows that for the title compound the IC50 of Hela is 0.175 μmol/mL and that of Bel7402 is 0.156 μmol/mL. 展开更多
关键词 (E)-4-tert-butyl-N-(2 4-dichorobenzylidene)-5-(1 2 4-triazl-1-yl)-thiazol-2-amine crystal structure synthesis antitumor activity
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Synthesis, Crystal Structure and Antitumor Activity of 4-tert-Butyl-N-(2-fluorophenyl)-5- (1H-1,2,4-triazol-1-yl)-thiazol-2-amine 被引量:1
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作者 李婉 叶姣 +2 位作者 沈芳 彭俊梅 胡艾希 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2012年第12期1782-1786,共5页
The title compound has been synthesized by the reaction of 1-bromo-3,3-dime- thyl- 1 - (1 H- 1,2,4-triazol- 1 -yl)butan-2-one with 1 -(2-fluorophenyl)thiourea, and its crystal struc- ture was determined by single-... The title compound has been synthesized by the reaction of 1-bromo-3,3-dime- thyl- 1 - (1 H- 1,2,4-triazol- 1 -yl)butan-2-one with 1 -(2-fluorophenyl)thiourea, and its crystal struc- ture was determined by single-crystal X-ray diffraction. The crystal belongs to the orthorhombic system, space group Pbca with a = 15.2568(6), b = 12.1533(5), c = 16.7307(7) A, Z = 8, V = 3102.2(2) A3, Mr = 317.39, Dc = 1.359 g/cm3, S = 1.05, μ = 0.223 mm-1, F(000) = 1328, the final R = 0.034 and wR = 0.097 for 2590 observed reflections (I 〉 2σ(I)). X-ray crystal structure presents the intramolecular N-H…N hydrogen bond, which plays an important role in stabilizing the crystal structure. In addition, the preliminary biological test on the title compound shows good antitumor activity, with IC50 of 0.122 μmol/mL against the Hela cell line. 展开更多
关键词 4-tert-butyl-N-(2-fluorophenyl)-5-(1H-1 2 4-triazol-1-yl)thiazol-2-amine SYNTHESIS crystal structure antitumor activity
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Synthesis, Crystal Structure and Antitumor Activity of 4-(tert-butyl)-5-(1H-1,2,4-triazol-1-yl)-N-(2-hydroxy-3,5-diiodinebenzyl)-thiazol-2-amine 被引量:1
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作者 叶姣 谢选青 +3 位作者 李康明 刘永超 孙利 胡艾希 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2015年第3期344-348,共5页
The title compound, 4-(tert-butyl)-5-(1 H- 1,2,4-triazol- 1 -yl)-N-(2-hydroxy-3,5-diio- dinebenzyl)thiazol-2-amine, was synthesized via the reduction of 4-(tert-butyl)-5-(1H-l,2,4- triazol-l-yl)-N-benzyliden... The title compound, 4-(tert-butyl)-5-(1 H- 1,2,4-triazol- 1 -yl)-N-(2-hydroxy-3,5-diio- dinebenzyl)thiazol-2-amine, was synthesized via the reduction of 4-(tert-butyl)-5-(1H-l,2,4- triazol-l-yl)-N-benzylidene-thiazol-2-amine with NaBH4, and its crystal structure was determined by single-crystal X-ray diffraction. The compound crystallizes in monoclinic system, space group P21/c with a = 7.91944(19), b = 10.5250(3), c = 24.4985(6) A, Z = 4, V = 2041.66(9) A3, Mr = 599.22, Dc = 1,949 Mg/m3, S = 1.120, p = 3.203 mm-1, F(000) = 1152, the final R = 0.0283 and wR = 0.0592 for 3490 observed reflections (I 〉 2σ(I)). X-ray analysis displays that the crystal water takes part in three intermolecular hydrogen bonds of O(2)-H(2A)…O(1), O(2)-H(2B)…N(I) and N(5)-H(5)…O(2), and an octatomic ring R^(8) is formed via intramolecular hydrogen bond of O(I)-H(IA)…N(4). Furthermore, the I…I contacts are involved in stabilizing the overall three-dimensional network structure. The preliminary biological test shows the title compound has good antitumor activity with the IC50 value of 26 μM against the Hela cell line. 展开更多
关键词 4-(tert-butyl)-5-(1H-1 2 4-triazol-1-yl)-N-(2-hydroxy-3-5-diiodinebenzyl)-thiazol-2-amine synthesis crystal structure antitumor activity
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A New and Efficient Method for the Synthesis of Pyrimido[2,1-<i>b</i>]Benzothiazole Derivatives
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作者 Fatemeh Chadegani Fatemeh Darviche Saeed Balalaie 《International Journal of Organic Chemistry》 2012年第1期31-37,共7页
The one-pot three-component reaction of 2-aminobenzothiazole, benzaldehyde derivatives and β-ketoester, β-diketone or malonate derivatives in solvent-free conditions provides the corresponding pyrimido [2,1-b] benzo... The one-pot three-component reaction of 2-aminobenzothiazole, benzaldehyde derivatives and β-ketoester, β-diketone or malonate derivatives in solvent-free conditions provides the corresponding pyrimido [2,1-b] benzothiazole derivatives at 60?C in 60% - 72% yields without using any catalyst in an optimistic time. 展开更多
关键词 4H-Pyrimido [2 1-b] BENZOthiazole Tandem Knoevenagel-Michael REACTION ONE-POT REACTION Green Chemistry
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Synthesis and Crystal Structure of Methyl 2-(Diphenylamino)-4-phenyl-1,3-thiazole-5-carboxylate
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作者 Ali Souldozi Seyed Hamid Reza Shojaei +2 位作者 Ali Ramazani Katarzyna lepokura Tadeusz Lis 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2013年第1期82-88,共7页
The title compound, methyl 2-(diphenylamino)-4-phenyl-1,3-thiazole-5-carboxylate, was synthesized and studied by single-crystal X-ray diffraction method. The structure of the product was confirmed by IR, 1H- and 13C... The title compound, methyl 2-(diphenylamino)-4-phenyl-1,3-thiazole-5-carboxylate, was synthesized and studied by single-crystal X-ray diffraction method. The structure of the product was confirmed by IR, 1H- and 13C-NMR spectroscopy and elemental analysis. These experimental studies were supported by quantum mechanical calculations. The structure was solved in monoclinic, space group P21/c with a = 9.573(3), b = 19.533(7), c = 9.876(3), β = 92.35(4)°, V = 1845.2(10)3, T = 85(2) K, Z = 4, R = 0.040 and wR = 0.089 for 6424 observed reflections with I2σ(I). 展开更多
关键词 single-crystal X-ray structure multi-component reaction methyl 2-(diphenylamino)-4-phenyl-1 3-thiazole-5-carboxylate benzoyl isothiocyanate DIPHENYLAMINE dimethyl acetylenedicarboxylate
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含有异噁唑的S-三唑[3,4-b]-1,3,4-噻二嗪、咪唑[2,1-b]-1,3,4-噻二唑和咪唑[2,1-b]-1,3,4-噁二唑衍生物的合成 被引量:9
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作者 刘方明 阿布拉江.克依木 +1 位作者 王厚勇 邵玲 《高等学校化学学报》 SCIE EI CAS CSCD 北大核心 2004年第9期1673-1675,共3页
Isoxazole derivatives were characterized by broad spectrum of biological activities, but the condensed heterocyclic compounds containing isoxazole were scarcely reported. In this paper, we studied the 1,3-dipolar cycl... Isoxazole derivatives were characterized by broad spectrum of biological activities, but the condensed heterocyclic compounds containing isoxazole were scarcely reported. In this paper, we studied the 1,3-dipolar cycloaddition of p-methoxybenzohydroxamoyl chloride with ethyl sodioacetoacetate to obtain a key intermediate 2. Through compound 2, fifteen novel S-triazolo-1,3,4-thiadiazines(5a-5e), imidazolo-1,3,4-thiadiazoles(9a-9e) and imidazolo-1,3,4-oxadiazoles(10a-10e) containing isoxazole, which have potentially useful biological activities, were synthesized. The structures of the products were confirmed by elemental analyses and spectral analysis. And the characteristic data of IR, 1H NMR and MS were explained reasonably. 展开更多
关键词 异噁唑 均三唑并噻二嗪 咪唑[2 1-b]-1 3 4-噻二唑 咪唑[2 1-b]-1 3 4-噁二唑
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含有1H-1,2,4-三唑咪唑[2,1-b]-1,3,4-噻二唑、S-三唑[3,4-b]-1,3,4-噻二唑衍生物的合成及生物活性 被引量:12
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作者 张艳 刘东 +4 位作者 戴朝峰 张自义 许鹏飞 惠新平 王勤 《高等学校化学学报》 SCIE EI CAS CSCD 北大核心 2002年第10期1882-1886,共5页
合成了 1 8个含有 1 H-1 ,2 ,4-三唑的咪唑 [2 ,1 -b]-1 ,3 ,4-噻二唑以及 S-三唑 [3 ,4-b]-1 ,3 ,4-噻二唑的稠杂环衍生物 ,经元素分析及谱学表征 ,探讨 2 ,5 ,6-三取代咪唑 [2 ,1 -b]-1 ,3 ,4-噻二唑的可能生成机制 .对大肠杆菌、绿... 合成了 1 8个含有 1 H-1 ,2 ,4-三唑的咪唑 [2 ,1 -b]-1 ,3 ,4-噻二唑以及 S-三唑 [3 ,4-b]-1 ,3 ,4-噻二唑的稠杂环衍生物 ,经元素分析及谱学表征 ,探讨 2 ,5 ,6-三取代咪唑 [2 ,1 -b]-1 ,3 ,4-噻二唑的可能生成机制 .对大肠杆菌、绿脓杆菌、枯草杆菌等初步抑菌试验证明 。 展开更多
关键词 合成 生物活性 1H-1 2 4-三唑 咪唑[2 1-b]-1 3 4-噻二唑 S-三唑[3 4-b]-1 3 4-噻二唑 抑菌活性
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小麦籽粒休眠Vp1-B1基因的等位变异检测与分离 被引量:3
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作者 张海萍 常成 +3 位作者 冯继明 殷波 司红起 马传喜 《分子植物育种》 CAS CSCD 2009年第2期297-302,共6页
Vp1基因是控制籽粒休眠性的重要基因之一,检测该基因的等位变异类型,可以进一步理解籽粒休眠以及穗发芽抗性的遗传控制机理。本文根据GenBank中小麦Vp1-B1基因序列设计特异引物检测我国小麦微核心种质以及地方品种和推广品种,结果表明,... Vp1基因是控制籽粒休眠性的重要基因之一,检测该基因的等位变异类型,可以进一步理解籽粒休眠以及穗发芽抗性的遗传控制机理。本文根据GenBank中小麦Vp1-B1基因序列设计特异引物检测我国小麦微核心种质以及地方品种和推广品种,结果表明,本研究除了发现已报道的3种等位变异类型,分别为Vp1-B1a、Vp1-B1b和Vp1-B1c,另外检测到一种新的变异类型,暂命名为Vp1-B1x。经改良的变性PAGE凝胶电泳检测以及序列比对分析表明,Vp1-B1x与Vp1-B1c基因的序列相似性最高,达99%;其在第3内含子区域发生"ATAT"4个碱基的插入以及4个SNP,但是该等位类型在所检测的品种中分布较少,其与籽粒休眠水平及穗发芽抗性之间的关系尚待进一步验证。 展开更多
关键词 小麦 休眠 收获前穗发芽 Vp1-b1
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1,4-二硝基呋咱并[3,4-b]哌嗪(DNFP)的合成 被引量:11
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作者 毕福强 王伯周 +2 位作者 王锡杰 熊存良 贾思媛 《含能材料》 EI CAS CSCD 北大核心 2009年第5期537-540,共4页
设计合成了高能量密度材料1,4-二硝基呋咱并[3,4-b]哌嗪(DNFP)。即以N,N′-二叔丁基乙二胺为起始原料,低温条件下与二氯乙二肟缩合环化生成1,4-二叔丁基哌嗪-2,3-二酮肟(PDO-tB),而后在氢氧化钠的乙二醇溶液中高温反应脱水环化得1,4-二... 设计合成了高能量密度材料1,4-二硝基呋咱并[3,4-b]哌嗪(DNFP)。即以N,N′-二叔丁基乙二胺为起始原料,低温条件下与二氯乙二肟缩合环化生成1,4-二叔丁基哌嗪-2,3-二酮肟(PDO-tB),而后在氢氧化钠的乙二醇溶液中高温反应脱水环化得1,4-二叔丁基呋咱并[3,4-b]哌嗪,经98%硝酸和硫酸的混酸体系硝解合成出DNFP,总收率32.6%,采用红外光谱、核磁共振谱、元素分析对DNFP和中间体结构进行了表征;改进了PDO-tB的合成工艺条件,加料方式由一次性加入改为缓慢滴加,并确定了适宜的冷浴温度为-18℃;研究了不同硝解体系对反应的影响,确定了适宜的硝解体系为硝硫混酸,硝解收率为61.7%。 展开更多
关键词 有机化学 1 4-二硝基呋咱并[3 4-b]哌嗪(DNFP) 呋咱 哌嗪 合成 表征
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溴氰菊酯降解菌Pseudomonas sp.P1-1-B3产酶条件的优化 被引量:3
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作者 刘丽花 王兆守 +3 位作者 陈小兰 徐敦明 郭英霞 邵宗泽 《厦门大学学报(自然科学版)》 CAS CSCD 北大核心 2010年第1期71-76,共6页
农药降解酶对去除农药残留污染具有良好的应用前景.从海洋沉积物中筛选到一株高产溴氰菊酯降解酶的菌株Pseudomonas sp.P1-1-B3,研究了碳源、氮源、pH值、培养温度、培养时间、接种量及溴氰菊酯对菌株产酶的影响.结果表明,降解菌产酶的... 农药降解酶对去除农药残留污染具有良好的应用前景.从海洋沉积物中筛选到一株高产溴氰菊酯降解酶的菌株Pseudomonas sp.P1-1-B3,研究了碳源、氮源、pH值、培养温度、培养时间、接种量及溴氰菊酯对菌株产酶的影响.结果表明,降解菌产酶的最适条件为:以可溶性淀粉作为碳源,m(蛋白胨):m(酵母浸膏)=2:1为氮源,pH 7.5,温度30℃,培养时间2 d,接种量3%,溴氰菊酯含量15μmol/L.在此条件下,菌株产酶的比活力最大为113.3 U/mg.该降解酶对溴氰菊酯的降解,在12 h内降解率达54.6%. 展开更多
关键词 溴氰菊酯 菌株Pseudomonas sp.P11-b3 降解酶 产酶条件 优化
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红芪多糖对糖尿病大鼠视网膜血小板反应蛋白-1和血小板源性生长因子-B表达的影响 被引量:11
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作者 张花治 金智生 +3 位作者 刘莹 颉瑞萍 赵建梅 高妍 《中国中医药信息杂志》 CAS CSCD 2017年第3期38-42,共5页
目的观察红芪多糖(HPS)对糖尿病大鼠视网膜血小板反应蛋白-1(TSP-1)和血小板源性生长因子-B(PDGF-B)表达的影响,探讨其对糖尿病视网膜病变的保护作用及可能机制。方法采用链脲佐菌素腹腔注射建立糖尿病模型。雄性Wistar大鼠随机分为模... 目的观察红芪多糖(HPS)对糖尿病大鼠视网膜血小板反应蛋白-1(TSP-1)和血小板源性生长因子-B(PDGF-B)表达的影响,探讨其对糖尿病视网膜病变的保护作用及可能机制。方法采用链脲佐菌素腹腔注射建立糖尿病模型。雄性Wistar大鼠随机分为模型组、多贝斯组和HPS高、中、低剂量组,另设正常组,每组10只。各给药组给予相应药物灌胃,模型组和正常组给予等量生理盐水灌胃,1次/d,连续8周。q RT-PCR和免疫组化检测TSP-1和PDGF-B m RNA和蛋白表达;HE染色镜下观察视网膜的结构。结果模型组视网膜各层结构清晰、完整,但外核层疏松变薄、排列紊乱,神经节细胞数量稍减少;各给药组较模型组明显好转。与正常组比较,模型组视网膜TSP-1 m RNA和蛋白表达明显降低(P<0.01),PDGF-B m RNA和蛋白表达明显升高(P<0.01);与模型组比较,各给药组TSP-1 m RNA和蛋白表达明显升高(P<0.05,P<0.01),PDGF-B m RNA和蛋白表达明显降低(P<0.01);HPS高剂量组与其余给药组比较,TSP-1和PDGF-B m RNA和蛋白表达差异有统计学意义(P<0.05,P<0.01)。结论 HPS可能通过升高糖尿病大鼠视网膜组织TSP-1的表达和降低PDGF-B的表达来阻遏糖尿病视网膜病变进程中新生血管生成及增殖,从而起到保护视网膜的作用。 展开更多
关键词 糖尿病 视网膜 红芪多糖 血小板反应蛋白-1 血小板源性生长因子-b 大鼠
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miR-375在子宫内膜癌HEC-1-B细胞中的生物学功能 被引量:4
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作者 叶文蔚 李甫钥 +1 位作者 叶夏斌 郑飞云 《实用医学杂志》 CAS 北大核心 2013年第2期177-180,共4页
目的:探讨miR-375在Ⅱ型子宫内膜癌中的表达及对HEC-1-B细胞增殖、凋亡的影响。方法:miRNA芯片分析Ⅱ型子宫内膜癌miRNA表达谱。利用lipofectamine 2000转染HEC-1-B细胞。实时荧光定量PCR检测转染后miR-375的表达。CCK-8检测转染后细胞... 目的:探讨miR-375在Ⅱ型子宫内膜癌中的表达及对HEC-1-B细胞增殖、凋亡的影响。方法:miRNA芯片分析Ⅱ型子宫内膜癌miRNA表达谱。利用lipofectamine 2000转染HEC-1-B细胞。实时荧光定量PCR检测转染后miR-375的表达。CCK-8检测转染后细胞增殖能力的改变。流式细胞仪检测细胞转染效率及转染后细胞凋亡情况。结果:miR-375在Ⅱ型子宫内膜癌组织中低表达。转染效率达73.43%。转染后实验组miR-375表达量较NC组和对照组明显增加(P<0.05)。实验组较NC组生长明显受抑(P<0.05)。实验组较NC组、对照组凋亡明显增加(P<0.05)。结论:初步证明miR-375抑制Ⅱ型子宫内膜癌细胞增殖并促进凋亡,可能成为Ⅱ型子宫内膜癌基因治疗的靶点。 展开更多
关键词 miR-375 HEC-1-b细胞 增殖 凋亡
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