A novel and efficient method was developed for the liquid-phase synthesis of Nj,4-disubstitutedbenzodiazepine-2,5-diones with 2-chloro-5-nitrobenzoic acid as initiating material via 4 step reactions containing esterif...A novel and efficient method was developed for the liquid-phase synthesis of Nj,4-disubstitutedbenzodiazepine-2,5-diones with 2-chloro-5-nitrobenzoic acid as initiating material via 4 step reactions containing esterifieation, ＂Ulmn reaction＂, acylation, alkylation and cyclization. The reaction conditions were mild and the overall yields of the products ranged from 45% to 71%.展开更多
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
基金Supported by the Natural Science Foundation of Hubei Province, China(No.2007ABA031)
文摘A novel and efficient method was developed for the liquid-phase synthesis of Nj,4-disubstitutedbenzodiazepine-2,5-diones with 2-chloro-5-nitrobenzoic acid as initiating material via 4 step reactions containing esterifieation, ＂Ulmn reaction＂, acylation, alkylation and cyclization. The reaction conditions were mild and the overall yields of the products ranged from 45% to 71%.
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。
