Antiviral activity of 3-(3,5-dimethylbenzyl)uracil derivatives against HIV-1 and HCMV.
Antiviral activity of 1,3-disubstituted uracil derivatives was evaluated against HIV-1 and HCMV. It appears that the nitrogen of the 1-cyanomethyl group is important for anti-HIV-1 activity, suggesting interaction with the amino acid residues of HIV-1 reverse transcriptase. 1-Arylmethyl derivatives also exhibited good anti-HIV-1 activity; and that of the 2- and 4-picolyl derivatives was particularly excellent.
Maruyama
Tokumi
T
Faculty of Pharmaceutical Sciences at Kagawa Campus, Tokushima Bunri University, Kagawa, Japan. maruyama@kph.bunri-u.ac.jp
Demizu
Yosuke
Y
Kozai
Shigetada
S
Witvrouw
Myriam
M
Pannecouque
Christophe
C
Balzarini
Jan
J
Snoecks
Robert
R
Andrei
Graciella
G
De Clercq
Erik
E
D000241:Adenosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D003587:Cytomegalovirus / Q000187:drug effects*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D012263:Ribonucleosides / Q000138:chemical synthesis* / Q000737:chemistry; D014498:Uracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
C527151:2'-O-(carbomoylmethyl)ribonucleoside H-phosphonate; C527152:2'-O-carbomoylmethyladenosine 3'-(thymidine 5'-phosphate); C527156:3-(3,5-dimethylbenzyl)uracil; D000998:Antiviral Agents; D012263:Ribonucleosides; D014498:Uracil; D000241:Adenosine