Synthesis of an Anti-AIDs Drug Delavirdine Derivate, Resdelasu

来源 :Chemical Research in Chinese Universities | 被引量 : 0次 | 上传用户:ymhd_hhxx
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
In view of the anti-HIV activities of delavirdine and resveratrol, a novel anti-AIDs drug Resdelasu, 1-{3-[(1-methyl-ethyl)amino]-2-pyridinyl}-4-{[5-(4-{5[(1E)-2-(hydroxyphenyl)ethenyl]-1,3-benzenedioyl-carbonylbu- tanoyl}amino)-1H-indol-2-yl]carbonyl}-piperazine was synthesized by linking the delavirdine derivative and resveratrol with succinic anhydride as the conjugated compound via two different routes. Its structure was confirmed by means of 1H NMR, 13C NMR, IR, MS, and elemental analysis. The route of esterification followed by amidation for synthesizing Resdelasu was simpler and gave a higher yield(46%) than that of amidation followed by esterification. It was proved that the method was efficient and convenient to prepare Resdelasu. The results of HIV-1 Reverse Transcriptase Assay and quantitative titration of HIV-1 via MAGI assay showed that a novel anti-AIDs drug, Resdelasu, had been synthesized. In view of the anti-HIV activities of delavirdine and resveratrol, a novel anti-AIDs drug Resdelasu, 1- {3 - [(1-methyl- ethyl) amino] -2-pyridinyl} -piperazine was synthesized by linking the delavirdine derivative and resveratrol (5) (1E) -2- (hydroxyphenyl) ethenyl] -1,3-benzenedioyl-carbonylbu- tanoyl} amino) -1H-indol-2-yl] carbonyl} with succinic anhydride as the conjugated compound via two different routes. Its structure was confirmed by 1H NMR, 13C NMR, IR, MS, and elemental analysis. The route of esterification followed by amidation for synthesizing Resdelasu was simpler and gave a higher yield (46%) than that of amidation followed by esterification. It was proved that the method was efficient and convenient to prepare Resdelasu. The results of HIV-1 Reverse Transcriptase Assay and quantitative titration of HIV-1 via MAGI assay showed that a novel anti -AIDs drug, Resdelasu, had been synthesized.
其他文献
财政资金管理的水平,关系到党的民生政策的落实,关系到群众的切身利益,关系到城乡统筹发展大局。近年来,荆门市漳河新区财政局漳河分局以“创新有为、全面提速”为基调;以落
案例:广东中山的陈先生花了70万元在中山市某汽车销售服务有限公司购买了一辆捷豹汽车,才行驶了8000公里,安全气囊就出现自爆。陈先生称,汽车肯定没有发生任何碰撞,事后报警
新中国成立以来,我国财政基本理论研究紧密结合实际,为实践服务并取得了长足的繁荣发展。不同财政基本理论之间看似简单无谓的概念之争,实则透露出研究范式及其认识论的差异,
据财政部11月27日消息,近日,财政部会同国家发展改革委、国家粮食局、中国农业发展银行印发通知,对采购东北地区2013年产粳稻、玉米实施费用补贴政策。通知明确,东北三省之外
甲状腺机能亢进症(以下简称甲亢),是一种自身免疫性疾病,老年人甲亢临床表现常复杂多样,易被误诊。我院近年来收治住院的老年甲亢患者中,入院时误诊7例,误诊率高达29%,现就误诊原因进行分
本文回顾概括了“十五”期间中国财政理论在若干基础领域的发展状况,并分析了其中存在的一些问题,进而提出了中国财政理论进一步发展需要研究的课题。 This paper reviews a
糖尿病外周血管病变是糖尿病的常见并发症,为了早期发现和及时治疗,我们采用足背静脉血气分析进行研究。报告如下。1资料与方法选糖尿病患者40例,分为两组。治疗组:20例,其中男11
会阴切口所处位置易发生感染、裂开 ,加之个体差异 ,患者对缝线排异反应重 ,痛苦大 ,故我院采用间断外“8”字全层缝合会阴侧切口 ,取得满意效果 ,现报告如下。1 资料与方法
为了提高掺杂染料的胆甾相液晶的激光效率,通过采用电击摩擦处理来改善染料掺杂胆甾相液晶内部分子的排列,结果表明对于不同厚度的胆甾相液晶样品,其内部分子排列的改善都能
Adipose tissue hypoxia has been recognized as the initiation of insulin resistance syndromes. The aim of the present study was to investigate the effects of man