The invention belongs to the technical field of medicine, in particular to a two aryl ketone hydrazone hydrazone derivative, a preparation method and an application thereof. The two aryl ketone hydrazone derivatives also comprise their pharmaceutically acceptable salts, their stereochemical isomers, their hydrates and solvates, their polymorphs or eutectic, their precursors and derivatives of the same biological functions. The preparation method is under the action of alkali salt, hydrazine, substituted hydrazine salt and two aryl pyrimidines in organic solvents were prepared by the reaction of the object; or, for hydrazine, hydrazine complexes substituted hydrazine substituted hydrazine complexes directly with two aryl pyrimidine reaction to obtain the target. The pharmacological test showed that the compounds in most of the wild type strains of HIV-1 replication and multiple drug resistant HIV-1 strains showed strong inhibitory activity, and some compounds on HIV-2 has strong inhibitory activity, is expected to become a candidate drug against HIV.
【技术实现步骤摘要】
本专利技术属医药
,具体涉及一种二芳基嘧啶酮腙衍生物及其制备方法和用途。
技术介绍
人类免疫缺陷病毒(HIV)导致的艾滋病(AIDS)是科学界难以攻克的顽症之一,呈现爆发流行趋势,给人类的生存和发展带来越来越严重的威胁。现有的药物有一定的疗效, 同时也存在着抗耐药性差、毒副作用大等问题。因此,寻找高效低毒的抗AIDS药物仍然是药物化学家面临的重大课题。目前抗AIDS药物的研究开发主要基于HIV生命循环过程的认识,其中,逆转录酶(RT)在基因组RNA的逆转录过程中起了重要作用,而且是HIV生命复制周期的早期阶段,所以RT成为抗AIDS药物研究的重要靶点之一。目前FDA批准的20种药物中有10种是以HIV RT作为靶点的。现有的抗HIV药物研究中,非核苷类逆转录酶抑制剂(NNRTIs)因其高效低毒等优点成为各国药物化学家关注的热点之一。目前,经美国FDA批准上市的抗HIV逆转录酶抑制剂有四种奈维拉平(Nevirapine)、德拉韦定(Delavirdine)、依非韦伦(Efavirenz),依曲韦林(etravirine)。经典的NNRTIs只作用于HIV-I ...
【技术保护点】
1.一种二芳基嘧啶酮腙衍生物,具有如下结构式(Ⅰ): Ⅰ其中,R1和R2分别独立地选自氢,羟基,卤素,任选被取代的C1-4烷基,任选被取代的C2-6烯基,任选被取代的C2-6炔基,C1-6烷氧基,氰基,硝基,氨基, -NH(OH)-,-N(R6)p-;R3、R4和R5分别独立地选自氢,羟基,卤素,任选被氰基或-C(=O)R6取代的C1-6烷基,C3-7环烷基,任选被一个或多个卤原子或氰基取代的C2-6烯基,任选被一个或多个卤原子或氰基取代的C2-6炔基, C1-6烷氧基,C1-6烷氧羰基,羧基,氰基,硝基,氨基,-NR7-,多卤代甲基, ...
【技术特征摘要】
还没有人留言评论。发表了对其他浏览者有用的留言会获得科技券。