Anti-viral guanidino-substituted compounds

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514432, 514459, 514460, 546247, 546243, 549 13, 549 28, 549417, 549419, 564236, A61K 3135, A61K 3138, A61K 31445, A61K 3117

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056271948

ABSTRACT:
Novel guanidino-substituted compounds are described having the following general formula (I): ##STR1## in which X may be carbon, oxygen, nitrogen or sulfur; R.sub.1 may be H, OH, linear or branched lower alkyl, lower alkoxy, lower (alkyl-substituted alkoxy), lower alkyl-amine, lower alkyl-thio, hydroxy substituted lower alkoxy, lower alkoxy-alkoxy substituted lower alkoxy, hydroxy substituted lower alkyl-amine, alkoxy substituted lower alkyl-amine and terminally guanidino-substituted linear of branched lower alkyl, lower alkoxy, lower (alkyl-substituted alkoxy), lower alkyl-amine or lower alkyl-thio; and R.sub.2 and R.sub.3 are independently one of linear or branched lower alkyl, alkoxy, alkyl-substituted alkoxy and alkylamine.
These compounds have been found to inhibit effectively herpesvirus replication. Particularly preferred compounds in accordance with formula (I) for this purpose are guanidino-substituted sugar derivatives.

REFERENCES:
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Nicolalou et al., "Design and synthesis of a peptidomimetic employing .beta.-D-glucose for scaffolding", Peptides: Chem Structure Biol., 11th An Pepetide Symp. (1990), pp. 881-884.
Shankar et al., "A novel application of benzotriazole methodology: reactions of polyhydroxylated bis-(benzotriazoyl) piperidines with mono and bidentate nucleophiles", Tetrahedron Letters, vol. 34, No. 45, (1993), pp. 7171-7174.

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