In vitro antiviral activity of 6-substituted 9-beta-D-ribofuranosylpurine 3', 5'-cyclic phosphates.

Abstract:

:A series of twelve recently synthesized 6-substituted derivatives of 9-beta-d-ribofuranosylpurine 3',5'-cyclic phosphate (RPcMP) were evaluated for in vitro antiviral activity, using inhibition of viral cytopathogenic effect as the primary parameter for evaluation. Inhibition of the development of intra- and extracellular virus titer was used as a secondary criterion with certain viruses. Five derivatives were considered to have significant antiviral activity. 6-Hydroxylamino-RPcMP was active against type 1 herpes simplex, cytomegalo-, and vaccinia viruses. 6-Thio-RPcMP was inhibitory to types 1 and 2 herpes simplex, cytomegalo-, vaccinia, and type 3 parainfluenza viruses. The 6-methylthio derivative was active against types 1 and 2 herpes simplex, cytomegalo-, and vaccinia viruses, and types 1A, 2, 8, and 13 rhinoviruses; alteration of this 6-substitution to 6-ethylthio or to 6-benzylthio weakened the herpes- and vaccinia virus activity of the compound, but each continued to have significant antirhinovirus activity. The effect of time of addition of 6-methylthio-RPcMP to type 1 herpes simplex virus-infected cells was determined; the compound was most active when added prior to the virus. Early removal of the compound from the infected cells markedly reduced its antiviral effectiveness.

authors

Sidwell RW,Huffman JH,Allen LB,Meyer RB Jr,Shuman DA,Simon LN,Robins RK

doi

10.1128/aac.5.6.652

subject

Has Abstract

pub_date

1974-06-01 00:00:00

pages

652-7

issue

6

eissn

0066-4804

issn

1098-6596

journal_volume

5

pub_type

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