Anti-
deoxyribonucleic acid virus activities of 3'-O-acyl derivatives of 2,2'-anhydro-1-beta-d-arabinofuranosyl
cytosine (
cyclo-C) and 1-beta-d-arabinofuranosylcytosine (
Ara-C) were evaluated by using an in vivo test system in mice. Among the derivatives tested, 3'-O-decanoyl
cyclo-C hydrochloride was the most effective against herpes simplex virus-induced
encephalitis in mice when the
drug was administered directly into infected brains of mice (target-organ treatment). A comparative study of the treatment of
herpetic encephalitis in mice with 3'O-decanoyl
cyclo-C and other
nucleosides, including
Ara-C,
9-beta-d-arabinofuranosyladenine (
Ara-A), and 5-iodo-2'-deoxyrudine (
IUdR), proved
Ara-A to be more efficacious than the other
nucleosides, followed by 3'-O-decanoyl
cyclo-C, which was more active than
Ara-C and
IUdR. Administration of 3'-O-acyl
cyclo-C's by
intraperitoneal injection, however, failed to demonstrate activity against
herpetic encephalitis in mice. The antivaccinial activity of 3'-O-decanoyl
cyclo-C was also compared with that of other compounds against
encephalitis and dermal tail lesions in mice caused by vaccinia virus
infection. Interaperitoneally administered 3'-O-decanoyl
cyclo-C and
Ara-C also showed no significant activity against the diseases. Under these test conditions,
N-methylisatin-beta-
thiosemicarbazone (
Marboran) was the most active compound, followed by
Ara-A.