Synthesis of N-substituted 3'-amino-3'-deoxythymidines and their biological evaluation against HIV.
Treatment of 3'-amino-3'-deoxythymidine (1) with carboxylic acid anhydrides afforded the corresponding acylamino derivatives 2a-f. Reaction of 1 with a variety of isothiocyanates led to the corresponding thioureido derivatives 3a-i. Also, conversion of 1 into 3'-carbylamino-3'-deoxythymidine (7) is reported. The compounds 2, 3, and 8 were evaluated for their anti-HIV activity in MT-4 cells, but did not show sufficient efficacy.
Motawia
M S
MS
Department of Chemistry, Odense University, Denmark.
Pedersen
E B
EB
Nielsen
C M
CM
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D015224:Dideoxynucleosides / Q000138:chemical synthesis* / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects*
D000998:Antiviral Agents; D015224:Dideoxynucleosides