Anti-HIV active naphthyl analogues of HEPT and DABO.
5-Ethyl-6-(1-naphthylmethyl)uracil and 5-ethyl-6-(1-naphthylmethyl)-2-thiouracil were alkylated to give, respectively. N-1 and S2, ethoxymethyl and methylthiomethyl uracil derivatives. 5-Ethyl-6-(1-naphthylmethyl)-2-thiouracil was also S2 alkylated with methyl bromoacetate. The products showed activity against HIV-1, and the N-1 alkylated derivatives were indeed highly active.
Danel
K
K
Department of Chemistry, Odense University, Denmark.
Nielsen
C
C
Pedersen
E B
EB
D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013889:Thiouracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D014498:Uracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
C107134:5-ethyl-6-(1-naphthylmethyl)-2-thiouracil; C107133:5-ethyl-6-(1-naphthylmethyl)uracil; D019380:Anti-HIV Agents; D014498:Uracil; D013889:Thiouracil