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Nucleic Acids Research, 1985, Vol. 13, No. 23 8519-8530
© 1985

Articles

The antiviral activity of tetrazole phosphonic acids and their analogues

D.W. Hutchinson and M. Naylor

Department of Chemistry, University of Warwick Coventry CV4 7AL, UK

Received October 11, 1985. Revised November 12, 1985. Accepted November 12, 1985.

5-(Phosphonomethyl)-lH-tetrazole and a number of related tetrazoles have been prepared and their effects on the replication of Herpes simplex Viruses–1 and –2 have been investigated as well as their abilities to inhibit the DNA polymerases induced by these viruses and the RNA transcriptase activity of influenza virus A. Contrary to an earlier report. 5-(phosphonomethyl)-1H-tetrazole was not an efficient inhibitor of the replication of HSV-1 and H8V-2 in tissue oulture. Analogues of 5-(phosphonomethyl)-lH-tetrazole were also devoid of significant antiviral activity. Only 5-(phosphonomethyl)-lH-tetrazole and 5-(thlophosphonomethyl)-lH-tetrazole inhibited the influenza virus transcriptase, and both were more effective as inhibitors than phosphonoacetic acid under the same conditions. The DNA polymerases induced by HSV-1 and HSV-2 were inhibited slightly by 5-(phosphonomethyl)-lH-tetrazole and to a lesser extent by its N-ethyl analogue and 3-(phosphonornethy)-lH-1,2,4-triazoie. None of these compounds were as effective as phosphonoacetic acid. 5-(Thiophosphonomethyl)-lH-tetrazole was a better inhibitor of the DNA polymerase induced by HSV-1 than 5-(phosphonomethyl)-1H-tetrazole.


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