Creating high-efifcient and environment-friendly pesticides is very important to produce the pollution free agriculture food and maintain the balance of the survival environmental of the human being. According to repo...Creating high-efifcient and environment-friendly pesticides is very important to produce the pollution free agriculture food and maintain the balance of the survival environmental of the human being. According to reports, camptothecin （CPT） and its derivatives are now being explored as a class of botanical insecticide in agriculture due to its novel mode of action. In order to improve the insecticidal activity of CPT, ten novel camptothecin （1） and 10-hydroxycamptothecin （2） derivatives （1a, 1b, 1c, 1d, 1e;2a, 2b, 2c, 2d, 2e） were designed and synthesized via esteriifcation with analogs of chrysanthemic acid, which have outstanding insecticidal activity. The results showed that compound 2a exhibited potent antifeeding effect and the best contact toxicity among the target compounds against the third-instar larvae of beet armyworm, Spodoptera exigua H＆#252;bner. Compound 2a was also found to be the most effective cytotoxic compound to the tested insect cell lines, IOZCAS-Spex-II, which were established from the fat bodies of S. exigua. It was proposed that the 10-hydroxyl group in the camptothecin derivatives is a key factor for the antifeeding activity of a compound. The nature of the substituents was considered the major factor in determining the insecticidal activity of these compounds.展开更多
In order to further confirm the biomimic properties of N-phosphoamino acids. A series of model compounds, analogue of phosphoryl amino acids, were synthesized and their biomimic mechanism was also investigated by NMR ...In order to further confirm the biomimic properties of N-phosphoamino acids. A series of model compounds, analogue of phosphoryl amino acids, were synthesized and their biomimic mechanism was also investigated by NMR and MS methods. The results indicated that the reactivity of phosphoryl biological small molecules was depended on the configuration, function groups and positions.展开更多
A convenient and easy method is described for the formation of carboxamides from carboxylic acids and primary amines in solventless conditions using infrared (IR) light. Thus, under IR light, cinnamic acid derivatives...A convenient and easy method is described for the formation of carboxamides from carboxylic acids and primary amines in solventless conditions using infrared (IR) light. Thus, under IR light, cinnamic acid derivatives and amines can produce yields ranging from 50% to 85% of the resulting amide.展开更多
目的观察参芎葡萄糖注射液联合依达拉奉注射液治疗进展性脑梗死(PCI)的疗效和安全性。方法将58例PCI患者随机分为2组。对照组28例予参芎葡萄糖注射液治疗;治疗组30例在对照组治疗基础上加用依达拉奉注射液治疗。2组均治疗14 d。观察2组...目的观察参芎葡萄糖注射液联合依达拉奉注射液治疗进展性脑梗死(PCI)的疗效和安全性。方法将58例PCI患者随机分为2组。对照组28例予参芎葡萄糖注射液治疗;治疗组30例在对照组治疗基础上加用依达拉奉注射液治疗。2组均治疗14 d。观察2组治疗前后神经功能缺损评分(NDS)、疗效,并检测肝肾功能、血尿常规及心电图。结果治疗组治疗后3 d NDS开始降低,治疗后14 d NDS明显降低(P<0.01),治疗后1个月NDS改善最为明显(P<0.01);对照组治疗后3 d NDS有增加趋势,但治疗后14 d、1个月NDS均有所下降(P<0.05)。2组治疗后任何1个阶段NDS比较差异均有统计学意义(P<0.05,P<0.01),尤其治疗后1个月时差异明显(P<0.01)。治疗组显效率66.7%,总有效率93.4%;对照组显效率42.9%,总有效率85.7%。2组显效率、总有效率比较差异均有统计学意义(P<0.05),治疗组疗效优于对照组。结论参芎葡萄糖注射液联合依达拉奉注射液治疗PCI疗效好,安全性高。展开更多
基金supported by the National Natural Science Foundation of China (31171878,31071707 and 31000851)
文摘Creating high-efifcient and environment-friendly pesticides is very important to produce the pollution free agriculture food and maintain the balance of the survival environmental of the human being. According to reports, camptothecin （CPT） and its derivatives are now being explored as a class of botanical insecticide in agriculture due to its novel mode of action. In order to improve the insecticidal activity of CPT, ten novel camptothecin （1） and 10-hydroxycamptothecin （2） derivatives （1a, 1b, 1c, 1d, 1e;2a, 2b, 2c, 2d, 2e） were designed and synthesized via esteriifcation with analogs of chrysanthemic acid, which have outstanding insecticidal activity. The results showed that compound 2a exhibited potent antifeeding effect and the best contact toxicity among the target compounds against the third-instar larvae of beet armyworm, Spodoptera exigua H＆#252;bner. Compound 2a was also found to be the most effective cytotoxic compound to the tested insect cell lines, IOZCAS-Spex-II, which were established from the fat bodies of S. exigua. It was proposed that the 10-hydroxyl group in the camptothecin derivatives is a key factor for the antifeeding activity of a compound. The nature of the substituents was considered the major factor in determining the insecticidal activity of these compounds.
文摘In order to further confirm the biomimic properties of N-phosphoamino acids. A series of model compounds, analogue of phosphoryl amino acids, were synthesized and their biomimic mechanism was also investigated by NMR and MS methods. The results indicated that the reactivity of phosphoryl biological small molecules was depended on the configuration, function groups and positions.
基金PAPIIT/UNAM Projects No.IN200614 and IT202015 and project PIAPI VC02 for partially supporting this worka part of the Project Catedra:Diseno de Sustancias Bioactivas of FESC-UNAM-2012.
文摘A convenient and easy method is described for the formation of carboxamides from carboxylic acids and primary amines in solventless conditions using infrared (IR) light. Thus, under IR light, cinnamic acid derivatives and amines can produce yields ranging from 50% to 85% of the resulting amide.
文摘目的观察参芎葡萄糖注射液联合依达拉奉注射液治疗进展性脑梗死(PCI)的疗效和安全性。方法将58例PCI患者随机分为2组。对照组28例予参芎葡萄糖注射液治疗;治疗组30例在对照组治疗基础上加用依达拉奉注射液治疗。2组均治疗14 d。观察2组治疗前后神经功能缺损评分(NDS)、疗效,并检测肝肾功能、血尿常规及心电图。结果治疗组治疗后3 d NDS开始降低,治疗后14 d NDS明显降低(P<0.01),治疗后1个月NDS改善最为明显(P<0.01);对照组治疗后3 d NDS有增加趋势,但治疗后14 d、1个月NDS均有所下降(P<0.05)。2组治疗后任何1个阶段NDS比较差异均有统计学意义(P<0.05,P<0.01),尤其治疗后1个月时差异明显(P<0.01)。治疗组显效率66.7%,总有效率93.4%;对照组显效率42.9%,总有效率85.7%。2组显效率、总有效率比较差异均有统计学意义(P<0.05),治疗组疗效优于对照组。结论参芎葡萄糖注射液联合依达拉奉注射液治疗PCI疗效好,安全性高。
