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Organoselenium compounds from purines: Synthesis of 6-arylselanylpurines with antioxidant and anticholinesterase activities and memory improvement effect
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2017-11-10 , DOI: 10.1016/j.bmc.2017.11.019
Luis Fernando B. Duarte , Renata L. Oliveira , Karline C. Rodrigues , Guilherme T. Voss , Benhur Godoi , Ricardo F. Schumacher , Gelson Perin , Ethel A. Wilhelm , Cristiane Luchese , Diego Alves

We describe here a simple method for the synthesis of 6-arylselanylpurines with antioxidant and anticholinesterase activities, and memory improvement effect. This class of compounds was synthesized in good yields by a reaction of 6-chloropurine with diaryl diselenides using NaBH4 as reducing agent and PEG-400 as solvent. Furthermore, the synthesized compounds were evaluated for their in vitro antioxidant and acetylcholinesterase (AChE) inhibitor activities. The best AChE inhibitor was assessed on the in vivo memory improvement. Our results demonstrated that the 6-((4-chlorophenyl)selanyl)-9H-purine and 6-(p-tolylselanyl)-9H-purine presented in vitro antioxidant effect. In addition, 6-((4-fluorophenyl)selanyl)-9H-purine inhibited the AChE activity and improved memory, being a promising therapeutic agent for the treatment of Alzheimer’s disease.



中文翻译:

嘌呤中的有机硒化合物:具有抗氧化剂和抗胆碱酯酶活性的6-芳基硒基嘌呤的合成和记忆改善作用

我们在这里描述了一种简单的合成具有抗氧化剂和抗胆碱酯酶活性的6-芳基硒基嘌呤的方法,并改善了记忆。通过使用NaBH 4作为还原剂和PEG-400作为溶剂,使6-氯嘌呤与二芳基二硒化物反应,可以高收率地合成这类化合物。此外,评估了合成的化合物的体外抗氧化剂和乙酰胆碱酯酶(AChE)抑制剂的活性。在体内记忆改善方面评估了最佳的AChE抑制剂。我们的结果表明,6-(((4-氯苯基)硒基)-9 H-嘌呤和6-(对甲苯基硒基)-9 H-嘌呤在体外呈递抗氧化作用。此外,6-(((4-氟苯基)硒基)-9 H-嘌呤抑制了AChE活性并改善了记忆力,是治疗阿尔茨海默氏病的有前途的治疗剂。

更新日期:2017-11-10
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