(核苷类似物的结构改造研究样本VIP专享

下载后可任意编辑摘要 核苷类似物作为临床抗病毒及抗肿瘤的药物讨论已有较长历史, 诞生了如齐多夫定( Zidovudine, AZT) 、 拉米夫定( Diethylamine) 等抗艾滋病及病毒性肝炎的药物, 对于此类疾病治疗有着重要的应用价值。但与此同时, 在核苷类似物的开发及临床应用过程中, 毒性及长期用药所产生的耐药性依旧制约着相关疾病的治愈。因此, 开发新型高效低毒的核苷类药物一直是人们讨论的热点。 核苷类化合物的修饰改造部位包括糖基和碱基部分, 其中大部分为糖基修饰改造的产物。糖基改造修饰的类型包括无环核苷, 脱氧核苷, 杂原子引入, 构型变化, 糖环大小的变化等。 在阅读文献并总结前人讨论的基础上, 本文的结构修饰方案是在对糖基修改的基础上, 接不同的碱基使其有不同的效果。关键词: 核苷类化合物; 碱基; 三叠氮下载后可任意编辑Abstract As a clinical drug studies of antiviral nucleoside analogues and anti-tumor has a long history, born as zidovudine (Zidovudine, AZT), (Diethylamine) and other anti-AIDS and hepatitis drugs, for the treatment of these diseases has important application value.At the same time, in the process of development and clinical application of the nucleoside analogs, chemical resistance and long-term toxicity of the drug remains a constraint generated to cure diseases.Therefore, the development of new and efficient low toxicity nucleoside drugs has been a hot topic of research. Modified nucleoside compounds reconstruction site, including glycosylation and the base portion, most of which is the transformation of the sugar-modified products. Modified Glycosylation type transformation include acyclic nucleosides, deoxynucleosid heteroatom introduced configuration changes, changes in the size of the sugar ring and the like. In reading the literature and on the basis of previous studies, structural modification programs on the basis of this paper is to modify the glycosylation, pick a different base it has a different ef...