Synthesis and antiviral activity of 1-substituted 3-(3,5-dimethylbenzyl)uracil against HIV-1.
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.
Maruyama
Tokumi
T
Faculty of Pharmaceutical Sciences at Kagawa Campus, Tokushima Bunri University, Shido, Sanuki City, Kagawa 769-2193, Japan.
Kozai
Shigetada
S
Demizu
Yosuke
Y
Witvrouw
Myriam
M
Pannecouque
Christophe
C
Balzarini
Jan
J
Snoeck
Robert
R
Andrei
Graciella
G
De Clercq
Erik
E
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D014498:Uracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
D000998:Antiviral Agents; D014498:Uracil