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Analogues of GLP-1 and Dipeptidy peptidase-Ⅳ inhibitors have a better prospect in the recent study.

其可被二肽基肽酶Ⅳ降解,半衰期极短,限制了其临床应用,目前研究GLP-1类似物及二肽基肽酶Ⅳ抑制剂有更好的应用前景。

However, it is still a vacancy for the metabolizability of resveratrol in the phenylalanine metabolism pathway.

但是由于白藜芦醇代谢在苯丙氨酸代谢途径中至今还是一个空白,因而与其衍生物和类似物的关系至今仍不够清晰。

The compounds in this paper have been licensed to Pico Pharmaceuticals, which plans to develop and initiate clinical trials of transition-state analogues.

本论文中的化合物已经授权给Pico制药公司,该公司计划开发并启动过渡态类似物的临床实验。

Aim According to the targets of 5-HT transporter and 5-HT2A receptor, a series of N -indolalkyl piperidine derivatives and their analogues were synthesized and tested for their biological activities.

摘要摘 要:目的以5-羟色胺转运体和5-HT2A受体为靶点,设计合成 N -吲哚烷基哌啶类化合物及其类似物,研究它们的体内外生物活性。

This Mets-analysis demonstrates that SSAs are effective in treatment of Graves ophthalmopathy and in reduction of proptosis, and it is equally effctive as glucocorticoid.

生长抑素类似物治疗Graves眼病有效,能减轻突眼的程度,其疗效与糖皮质激素的作用相当。

It's has been reported that lactoquinomycin and frenolicin B, analogues of kalamycin, can inhibit AKT for the pyran naphthoquinone skeleton they have. We found that although kalamycin has pyran naphthoquinone skeleton, but did not suppress AKT and its downstream signal system, then we make a sytematic analysis on the in vitro anti-tumor effect and mechanism of kalamycin.

有报道其类似物lactoquinomycin和frenolicin B是肿瘤靶点AKT抑制剂,并由此推断吡喃萘醌骨架在AKT抑制过程中发挥主要作用,我们发现虽然卡拉霉素含有吡喃萘醌骨架,但是并不抑制AKT及其下游信号系统;继而对卡拉霉素的体外抗肿瘤作用及其机理进行了系统的分析。

Synthesis of target compounds namely: to vanillic acid as the starting material with methanol under reflux conditions for 4 - hydroxy -3 - p-methyl, then ether, and nitration, reduction, cyclization reaction 6 - methoxy -7 - benzyloxy-quinazoline -4 - one, and then by the chloride in place of aniline, benzyloxy-off, such as etherification reaction of the target compounds; target compounds with the second and third occurrence of substitution reactions of amines by the TM1, that is, 4 - amino-benzene -6 - methoxy -7 - [2 - hydroxy -3 -(N, N-diethyl amino) oxy c] quinazoline; with ether occurred Ornidazole reaction of TM2, namely, 4 - amino-benzene -6 - methoxy -7 - [2 - hydroxy -3 -(2 - methyl -5 - nitroimidazole) C oxy] quinazoline.

本论文以嘌呤类似物喹唑啉为母核,分别在其4位和7位引入结构多样的取代苯氨基和柔性侧链,设计了一系列4-取代苯胺基-6-甲氧基-7-(2-羟基取代丙氧基)喹唑啉类化合物。目标化合物的合成即:以香草酸为起始原料,与甲醇回流条件下得到4-羟基-3-甲氧基苯甲酸甲酯,然后经过醚化、硝化、还原、环合反应得到6-甲氧基-7-苄氧基喹唑啉-4-酮,然后再经氯化、取代苯胺、脱苄氧基、醚化等反应得到目标化合物;目标化合物与二乙胺发生胺取代反应得到了TM1,即4-苯氨基-6-甲氧基-7-[2-羟基-3-丙氧基]喹唑啉;通过与奥硝唑发生醚化反应得到TM2,即4-苯氨基-6-甲氧基-7-[2-羟基-3-(2-甲基-5-硝基咪唑)丙氧基]喹唑啉。

The research of recent years shows that phloem loading and unloading of plant photoassimilate both have symplasmic and apoplasmic pathways. Sugars transported by loading mainly are:(1) raffinose and its analogue,(2) sucrose.

近年来研究表明,植物体内光合同化物的韧皮部装载和卸出均有共质体途径和质外体途径,装载转运的糖类主要有:⑴棉子糖及其类似物;⑵蔗糖。

Then, a series of saponin analogues were designed and synthesized as the major work in this dissertation.

重点设计并合成了一系列皂苷类似物,并对其进行了体外活性研究。

A single systemic injection of resiniferatoxin , an ultrapotent analog of capsaicin, produced a long-lasting, reversible blockade of adjuvant-induced thermal hyperalgesia and reduction of early edema in the adult rat. Depletion of mast cell granules in peripheral connective tissues with secretagogue compound 48/80 also reduced the hyperalgesia and early edema to some extent. Co-pretreatment with RTX and compound48/80 had the similar effects as that of RTX treated alone. After unilateral surgical sympathectomy, the thermal hyperalgasia and edema were both significantly enhanced.

成年鼠一次性注射辣椒素类似物resiniferatoxin后,长时程、可逆性阻断了CFA所致热痛过敏的发展并削弱了早期炎性水肿;用促脱颗粒剂compound48/80慢性耗竭外周结缔组织肥大细胞内分泌颗粒后,也部分削弱了热痛过敏及早期水肿的形成;RTX与compound48/80共同处理对热痛过敏及水肿有与RTX单独处理相近程度及时程的影响;单侧交感链切除显著易化了炎性热痛过敏及水肿。

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