转录反式激活因子(trans-activator of transcription,Tat)在HIV-1的转录中起着重要的调控作用,针对HIV-1 Tat中的β-转角结构,采用2H-1,4-苯并二氮-2-酮作为β-转角肽链骨架的模拟结构,分别以对硝基氯苯/苯乙腈、对甲基苯胺/苯甲酰氯...转录反式激活因子(trans-activator of transcription,Tat)在HIV-1的转录中起着重要的调控作用,针对HIV-1 Tat中的β-转角结构,采用2H-1,4-苯并二氮-2-酮作为β-转角肽链骨架的模拟结构,分别以对硝基氯苯/苯乙腈、对甲基苯胺/苯甲酰氯以及硝西泮为起始原料,采用不同合成路线得到了19个2H-1,4-苯并二氮-2-酮类化合物(10～18、21～24、26～31)。初步活性评价表明,化合物30在没有明显细胞毒作用的浓度下对Tat介导的荧光素酶的表达显示了较好的抑制作用,其半数有效浓度EC50为25.0μmol·L-1。展开更多
Eight novel 5,7-disubstituted-2-{5-methyl-3-（4-trifluoromethylphenyl）isoxazol-4-ylcarbonylimino}-2H-1,2,4-thiadiazolo[2,3- a]pyrimidines were synthesized by multi-step reactions in yields 68-85%.Reactions were carri...Eight novel 5,7-disubstituted-2-{5-methyl-3-（4-trifluoromethylphenyl）isoxazol-4-ylcarbonylimino}-2H-1,2,4-thiadiazolo[2,3- a]pyrimidines were synthesized by multi-step reactions in yields 68-85%.Reactions were carried out either by ultrasound irradiation or conventional method,and found it was faster and more efficient under ultrasonic irradiation.Preliminary herbicidal activities against Echinochloa crus-galli,Digitaria sanguinalis and Chenopodium serotinum were also evaluated by flat-utensil method,and the results indicated that the target compounds exhibited significant activities,some were even higher than the control herbicide.展开更多
文摘转录反式激活因子(trans-activator of transcription,Tat)在HIV-1的转录中起着重要的调控作用,针对HIV-1 Tat中的β-转角结构,采用2H-1,4-苯并二氮-2-酮作为β-转角肽链骨架的模拟结构,分别以对硝基氯苯/苯乙腈、对甲基苯胺/苯甲酰氯以及硝西泮为起始原料,采用不同合成路线得到了19个2H-1,4-苯并二氮-2-酮类化合物(10～18、21～24、26～31)。初步活性评价表明,化合物30在没有明显细胞毒作用的浓度下对Tat介导的荧光素酶的表达显示了较好的抑制作用,其半数有效浓度EC50为25.0μmol·L-1。
基金supported by Shandong Province Natural Science Foundation(NoZR2009BM044)
文摘Eight novel 5,7-disubstituted-2-{5-methyl-3-（4-trifluoromethylphenyl）isoxazol-4-ylcarbonylimino}-2H-1,2,4-thiadiazolo[2,3- a]pyrimidines were synthesized by multi-step reactions in yields 68-85%.Reactions were carried out either by ultrasound irradiation or conventional method,and found it was faster and more efficient under ultrasonic irradiation.Preliminary herbicidal activities against Echinochloa crus-galli,Digitaria sanguinalis and Chenopodium serotinum were also evaluated by flat-utensil method,and the results indicated that the target compounds exhibited significant activities,some were even higher than the control herbicide.
