Synthesis and anti-herpes virus activity of 2'-deoxy-4'-thiopyrimidine nucleosides

J Med Chem. 1996 Feb 2;39(3):789-95. doi: 10.1021/jm950029r.

S G Rahim ¹, N Trivedi, M V Bogunovic-Batchelor, G W Hardy, G Mills, J W Selway, W Snowden, E Littler, P L Coe, I Basnak, R F Whale, R T Walker

Affiliations

Affiliation

1 Wellcome Research Laboratories, Beckenham, Kent, U.K.

PMID: 8576922 DOI: 10.1021/jm950029r

Abstract

A series of 5-substituted 2'-deoxy-4'-thiopyrimidine nucleosides was synthesized and evaluated as potential Antiviral agents. A number of analogues such as 2'-deoxy-5-propyl-4'-thiouridine (3ii), 2'-deoxy-5-isopropyl-4'-thiouridine (3iii), 5-cyclopropyl-2'-deoxy-4'-thiouridine (3iv), 2'-deoxy-4'-thio-5-vinyluridine (3viii), and 5-(2-chloroethyl)-2'-deoxy-4'-thiouridine (3xx) were found to be highly active against herpes simplex virus type-1 (HSV-1) and varicella zoster virus (VZV) in vitro with no significant cytotoxicity. The compound with the broadest spectrum of activity was 2'-deoxy-5-ethyl-4'-thiouridine (3i) which showed significant activity against HSV-1, HSV-2, and VZV.

Name
Email *

	Sorry, but the email address you supplied was invalid.