68027-76-9Relevant academic research and scientific papers
Solid phase synthesis of diamino-substituted pyrimidines
Barillari, Caterina,Barlocco, Daniela,Raveglia, Luca F.
, p. 4737 - 4741 (2001)
2,4- and 4,6-Diamino-substituted pyrimidines are known for their biological activity in many therapeutic areas. A novel solid-phase synthesis of this class of compounds by nucleophilic aromatic substitution has been set up and the reactivity of differently substituted solid-supported pyrimidines with properly selected amines has been studied. Using this methodology a small library of diamino-substituted pyrimidines has been prepared. Wiley-VCH Verlag GmbH, 2001.
Substituted pyrimidine compounds and application thereof
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Paragraph 0108; 0109; 0110; 0111, (2016/10/08)
The invention relates to substituted pyrimidine compounds and an application thereof. The substituted pyrimidine compounds are compounds shown in a formula I (the specific structure is shown in the specification or claims), stereoisomers of the compounds or pharmaceutically acceptable salts of the compounds. An in-vitro activity test proves that the substituted pyrimidine compounds have cholinesterase inhibiting activity, metal ion chelation, inhibition of generation of metal ion induced free radicals, inhibition of metal ion induced Abeta aggregation and the like. Therefore, the substituted pyrimidine compounds are expected to be used for preparing Alzheimer's disease treating and/or preventing drugs.
Development of Multifunctional Pyrimidinylthiourea Derivatives as Potential Anti-Alzheimer Agents
Li, Xiaokang,Wang, Huan,Lu, Zhengyu,Zheng, Xinyu,Ni, Wei,Zhu, Jin,Fu, Yan,Lian, Fulin,Zhang, Naixia,Li, Jian,Zhang, Haiyan,Mao, Fei
, p. 8326 - 8344 (2016/10/03)
Starting from a screening-hit compound, via structure modifications and optimizations, a series of nonfused and nonassembly pyrimidinylthiourea derivatives (2-5) was designed, synthesized, and evaluated as novel multifunctional agents against Alzheimer's disease. Biological activity results demonstrated that compounds 5r and 5t exhibited potent inhibition and excellent selectivity toward acetylcholinesterase (AChE, 5r, IC50 = 0.204 μM, SI > 196; 5t, IC50 = 0.067 μM, SI > 597), specific metal-chelating ability, significant antioxidant effects, modulation of metal-induced Aβ aggregation, inhibition of ROS production by copper redox cycle, low cytotoxicity, and moderate neuroprotection to human neuroblastoma SH-SY5Y cells. Moreover, compound 5r displayed appropriate blood-brain barrier (BBB) permeability both in vitro and in vivo and could improve memory and cognitive function of scopolamine-induced amnesia mice. The multifunctional profiles of 5r and its effectivity in AD mice highlight these structurally distinct pyrimidinylthiourea derivatives as prospective prototypes in the research of innovative multifunctional drugs for Alzheimer's disease.
