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化合物

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Bicyclic compounds containing a phenyl or pyridyl ring fused to a cycloalkyl or heterocyclic ring, to which is attached a 5-membered heterocyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

本发明涉及含有连接在5元杂环上的稠合至环烷基或者杂环的苯基或者吡啶基环的二环化合物,包括其药学上可接受的盐和前药,它们是G蛋白偶联受体40(GPR40)激动剂并且可以用作治疗性化合物,特别是在2型糖尿病和与这些疾病相关的症状中用作治疗性化合物,这些症状包括肥胖病和脂质疾病,比如混合或者糖尿病型血脂异常症、血脂质过多、高胆甾醇血和高甘油三酯血症。

The crystal structures proved that pyrrolic amide moiety could be as a new kind of hydrogen bonding building block and has potential application in the design of supramolecular structure.

首次在吡咯酰胺化合物的单晶结构中发现了该类化合物的一种新的氢键组装模式,为更合理地利用吡咯酰胺化合物去设计组装体打下了理论基础。

Halogenated aromatic compounds with great q〓(the most negative net atomic charges on an atom of the molecule), ENC (electron-nuclear attraction energy of the one-center term for the carbon atoms of the weakest carbon-halogen bond), qc (thenet atomic charges on the carbon atom of the weakest carbon-halogen bond) and E〓 tend to be reductively dehalogenated slow, while halogenated aromatic compounds with high values of △E (the difference of front-line orbital energy), EEC (electron-electron repulsion energy of the one-center term for the carbon atoms of the weakest carbon-halogen bond), Mw, q〓 and α tend to be reductively dehalogenated fast.

卤代芳烃化合物的整个分子的最负的原子净电荷,键序最小的碳卤键中碳原子的单中心项电子-核吸引能,该碳-卤键上碳原子的净电荷和E〓与该卤代芳烃化合物还原脱卤的速率常数负相关;而前线轨道间隙能,键序最小的碳卤键中碳原子的单中心项电子-电子推斥能,Mw,q〓和α与该卤代芳烃化合物还原脱卤的速率常数正相关。

Compound 1 is a new compound and the others were isolated from Rhamnus crenatus for tile first time.

化合物1为新化合物,其余化合物均为首次从该植物中分离得到。

The result expressed that under the concentration of 0.2mg/mL, the 6 compounds are all active to Sarcina lutea, ME-1, MT-6, MT-land MT-7 are active to Bacillus megaterium, to Escherichia coli, only MT-2 is active. The dimeric natural products are intensively existed in botany, most of them have the obvious biological activities. They have been concentrated on in recent years, and they are one of the compounds to which are enjoyed great popularity in natural product.

结果表明,在浓度为0.2mg/mL的条件下,六种化合物对藤黄八叠球菌均具有明显抑制作用,ME-1、MT-6、MT-1、MT-7对巨大芽孢杆菌有抑制作用,MT-2对大肠杆菌有抑制作用,对绿脓杆菌和枯草芽孢杆菌六种成分均无抑制作用;二聚体化合物在植物界广泛存在,多数二聚体天然产物具有显著的生物活性,引起人们的重视,是天然产物化学界研究的热门化合物之一。

Additionally, 75 volatile chemical constituents have been identified from the petroleum ether extracted part by capillary GC-MS, and the relative percentages of them are determined by GC method. The result showed that the volatile constituents of Musella lasiocarpa mainly includes advanced alkane, aliphatic acid and ester, aldehyde, ketone, aromatic and its heterocyclic compounds. With the compounds that have been isolated and identified from Musella lasiocarpa, the biogenensis pathway of new compound MT-3 is approached. Furthermore, the bacteriostasis of the 6 compounds to Escherichia coil, Pseudomonas aerusinosa, Bacillus megaterium, Sarcina lutea and Bacillus subtilic are determined by flat dilution method.

此外,从其石油醚萃取部分用毛细管色谱法分析鉴定出75种挥发性化学成分,并测定了各组分的相对百分含量,结果表明,地涌金莲挥发性化学成分以高级烷烃、高级脂肪酸酯及醛、酮、芳香和芳香杂环化合物为主;根据从地涌金莲中鉴出和分离得到的化合物,探讨了新结构化合物MT-3的生源代谢途径;采用平板稀释法测定了地涌金莲中六种化学成分对大肠杆菌、绿脓杆菌、巨大芽孢杆菌、藤黄八叠球菌和枯草芽孢杆菌的抑菌作用。

The preliminary bioassays indicated that, at 500 g/mL, 1-(o-tolyl-4-(4-chloro-3-ethyl-1-methylpyrazol-5-ylcarbonyl)semicarbazide (4g) and 1-(2,4-dimethyl- phenyl)-4-(4-chloro-3-ethyl-1-methylpyrazol-5-ylcarbonyl)semicarbazide (4k) showed inhibitory activities 90% and 80% against Blumeria graminis, respectively; and at 25 g/mL, 4-phenyl-4-(4-chloro-3-ethyl-1- methylpyrazol-5-ylcarbonylsemicarbazide (4c) showed inhibitory activity 70.1% against Botrytis cinerea and 1-2-nitro-phenyl-4-(4-chloro-3-ethyl-1-methylpyrazol-5-ylcarbonylsemicarbazide (4d) showed inhibi-tory activitiy 51.3% against Pyricularia oryzae.

初步生物活性实验结果表明,在500 mg/mL浓度下,化合物1-(4-氯-3-乙基-1-甲基-1H-吡唑-5-甲酰基)-4-(2-甲基苯基)氨基脲(4g), 1-(4-氯-3-乙基-1-甲基-1H-吡唑-5-甲酰基)-4-(2,4-二甲基苯基)氨基脲(4k)对小麦白粉病菌的抑制率分别达到90%和80%;在25 mg/mL浓度下,化合物1-(4-氯-3-乙基-1-甲基-1H-吡唑-5-甲酰基)-4-苯基氨基脲(4c)对黄瓜灰霉病菌的抑制率达到70.1%;化合物1-(4-氯-3-乙基-1-甲基-1H-吡唑-5-甲酰基)-4-苯基氨基脲(4c)和1-(4-氯-3-乙基-1-甲基-1H-吡唑-5-甲酰基)-4-(2-硝基苯基)氨基脲(4d)对稻瘟病菌的抑制率均达到51.3%。

The segments 〓 and 〓 were coupled via Cadiot-Chodkiewcz reaction to afford the intermediate 〓. After the silyl protective groups were removed by TBAF from 〓, we accomplished the stereoselective total synthesis of the target molecule-(11S, 16S)- Oplopandiol Acetate〓.

通过中间体化合物〓和〓的Cadiot-Chodkiewiza炔炔偶联反应得到了中间体化合物〓,再用TBAF脱除保护基完成了目标化合物〓的首次全合成,确证其绝对构型为11S、16S。

Synthesis and Thermoelectric Properties of Nano-Skutterudite Compounds by Chemical Methods;2. Thermoelectric Properties and Nanostructuring of Skutterudites;3. The synthesis approaches and its characteristic of skutterudite compounds,such as smelting,solid-state reaction,mechanical alloying and spark plasma sintering etc were reviewed.

回顾了熔融法、固相反应法、机械合金化和放电等离子烧结技术等方钴矿热电材料的制备方法及其特点,重点阐述了在方钴矿化合物中固溶Fe,Ni等元素,以及在方钴矿化合物中填充碱土或稀土元素对热电性能的改进;同时介绍了低维化对方钴矿化合物的热电传输特性的影响。

The main purpose of this thesis was the chemistry composition analysis and research of Sorbus tianschanica . This thesis first made preparation of an experiment in detail to the fruit of the sorbus tianschanica to Xinjiang ,then mainly aimed to research flavonoid compounds of the sorbus tianschanica.

本论文主要对新疆天山花楸的黄酮类化合物进行了研究,首先对天山花楸的果实进行了预实验,然后对天山花楸枝叶的黄酮类化合物进行了定性研究及对其不同有效部位的黄酮类化合物进行了较为详细的定量研究。

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According to the clear water experiment, aeration performance of the new equipment is good with high total oxygen transfer coefficient and oxygen utilization ratio.

曝气设备的动力效率在叶轮转速为120rpm~150rpm时取得最大值,此时氧利用率和充氧能力也具有较高值。

The environmental stability of that world - including its crushing pressures and icy darkness - means that some of its most famous inhabitants have survived for eons as evolutionary throwbacks, their bodies undergoing little change.

稳定的海底环境─包括能把人压扁的压力和冰冷的黑暗─意谓海底某些最知名的栖居生物已以演化返祖的样态活了万世,形体几无变化。

When I was in school, the rabbi explained everythingin the Bible two different ways.

当我上学的时候,老师解释《圣经》用两种不同的方法。