A series of pyrimidine conjugates containing a fragment of racemic 7,8-difluoro-3,4-dihydro-3-methyl-2 H -[1,4]benzoxazine and its ( S )-enantiomer attached via a 6-aminohexanoyl fragment were synthesized by the reaction of nucleophilic substitution of chlorine in various chloropyrimidines. The structures of the synthesized compounds were confirmed by ^{1}H, ^{19}F, and ^{13}C NMR spectral data. Enantiomeric purity of optically active derivatives was confirmed by chiral HPLC. Antiviral evaluation of the synthesized compounds has shown that the replacement of purine with a pyrimidine fragment leads to a decrease in the anti-herpesvirus activity compared to the lead compound, purine conjugate. The studied compounds did not exhibit significant activity against influenza A (H1N1) virus.
【저자키워드】 Influenza virus, antiviral activity, HSV-1, pyrimidine, purine, 7,8-difluoro-3,4-dihydro-3-methyl-2H-[1,4]benzoxazine,