当前位置: X-MOL 学术Nucleosides Nucleotides Nucleic Acids › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Efficient one-pot, three-component procedure to prepare new α-aminophosphonate and phosphonic acid acyclic nucleosides
Nucleosides, Nucleotides & Nucleic Acids ( IF 1.3 ) Pub Date : 2020-10-08 , DOI: 10.1080/15257770.2020.1826516
Laila Baddi 1 , Driss Ouzebla 1 , Az-Eddine El Mansouri 1 , Michael Smietana 2 , Jean-Jacques Vasseur 2 , Hassan B. Lazrek 1
Affiliation  

Abstract An efficient one-pot three-component Kabachnik–Fields reaction of aldehydes (acyclic nucleosides), amines (or amino acid), and triethyl phosphite proceeded for the synthesis of aminophosphonates using natural phosphate coated with iodine (I2@NP) as a catalyst. The novel α-aminophosphonate and phosphonic acid acyclic nucleosides were tested for their anti-HCV and anti-HIV activities. The molecular docking showed that the non-activity of these compounds could be due to the absence of hydrophobic pharmacophores.

中文翻译:

制备新型α-氨基膦酸酯和膦酸无环核苷的高效一锅三组分程序

摘要 醛(无环核苷)、胺(或氨基酸)和亚磷酸三乙酯的高效一锅三组分 Kabachnik-Fields 反应用于合成氨基膦酸酯,使用碘包覆的天然磷酸盐 (I2@NP) 作为催化剂. 测试了新型 α-氨基膦酸酯和膦酸无环核苷的抗 HCV 和抗 HIV 活性。分子对接表明,这些化合物的非活性可能是由于不存在疏水性药效团。
更新日期:2020-10-08
down
wechat
bug