In vitro antiherpesviral activity of 5-alkyl derivatives of 1-beta-D-arabinofuranosyluracil.

Abstract

Several 5-alkyl derivatives of 1-beta-d-arabinofuranosyluracil (araU) were tested for antiherpesviral activity and inhibitory action on cell growth in human embryonic lung fibroblasts. 1-beta-d-Arabinofuranosylcytosine, 9-beta-d-arabinofuranosyladenine, and 5-iododeoxyuridine (IUdR) were included as reference materials. Among the 5-alkyl derivatives of araU, arabinosylthymine was the most active, followed by 5-ethyl- and 5-propyl-araU. 5-Ethyl-araU was as active as IUdR and more active than 9-beta-d-arabinofuranosyladenine against herpes simplex virus (HSV) type 1 and did not inhibit cell growth at a concentration as high as 1,000 mug/ml. 5-Butyl- and 5-methoxymethyl-araU, as well as araU, exhibited relatively low activity. The araU derivatives tested were as active against HSV WT-34, an isolate from a patient with keratitis, as against HSV type 1. Against an IUdR-resistant isolate, HSV WT-20, arabinosylthymine was less inhibitory than IUdR. Deoxyribonucleic acid synthesis in HSV type 1-infected cells was markedly inhibited by arabinosylthymine, IUdR, and 5-ethyl-araU, whereas cellular deoxyribonucleic acid synthesis in uninfected cells was significantly inhibited by IUdR but not by arabinosylthymine or 5-ethyl-araU.

• Authors: H Machida, S Sakata, A Kuninaka, H Yoshino, C Nakayama, M Saneyoshi
• Journal: Antimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 16 Issue 2 Pg. 158-63 (Aug 1979) ISSN: 0066-4804 [Print] United States
• PMID: 485126 (Publication Type: Journal Article)

Chemical References

• Arabinofuranosyluracil
• DNA
• Thymidine
• Uridine

Topics

• Arabinofuranosyluracil (analogs & derivatives, pharmacology)
• Cell Division (drug effects)
• Cytopathogenic Effect, Viral (drug effects)
• DNA (biosynthesis)
• Herpes Simplex (drug therapy)
• Thymidine (metabolism)
• Uridine (analogs & derivatives)