Maruyama Tokumi, Kozai Shigetada, Demizu Yosuke, Witvrouw Myriam, Pannecouque Christophe, Balzarini Jan, Snoeck Robert, Andrei Graciella, De Clercq Erik
Faculty of Pharmaceutical Sciences at Kagawa Campus, Tokushima Bunri University, Shido, Sanuki City, Kagawa 769-2193, Japan.
Nucleic Acids Symp Ser (Oxf). 2004(48):3-4. doi: 10.1093/nass/48.1.3.
1,3-disubstituted uracils were obtained from uracil by the stepwise alkylation at N-1 and N-3 position with alkyl halide/alkali or alcohol under Mitsunobu conditions. The antiviral activity against HIV-1 of these compounds was examined to find that 1-cyanomethyl-3-(3,5-dimethylbenzyl)uracil and 1-phenyl-3-(3,5-dimethyl-benzyl)uracil showed powerful inhibition.
通过在米氏条件下用卤代烷/碱或醇对尿嘧啶的N-1和N-3位进行逐步烷基化反应，从尿嘧啶制得1,3-二取代尿嘧啶。对这些化合物针对HIV-1的抗病毒活性进行了检测，发现1-氰基甲基-3-(3,5-二甲基苄基)尿嘧啶和1-苯基-3-(3,5-二甲基苄基)尿嘧啶表现出强大的抑制作用。
