[Experimental results with systematically synthetized substances for antiviral chemotherapy / 4th communication: The role of physical binding in the synthesis of antiviral chemotherapeutics and its influence on potential mutagenic effects (author's transl)].
13 antiviral substances containing specific hydrogen bridge linkage systems out of the classes of 2-substituted 4-phenylthiazoles, 4-phenylimidazoles and indandiones-(1,3) were tested for their mutagenic potency in the host-mediated assay, in bone marrow of rats, in spermatogonia of mice and in the micronucleus test of rats. Only one substance, N1-methyl-N2-[4-phenylthiazolyl-(2)]-urea, was found to be mutagenic. This fact substantiates the hypothesis that the antiviral effectiveness of the substances is not caused by a chemical change in the coding system but by forming "physical" linkages like hydrogen bridge complexes with coding structures. Altogether 159 compounds of very different structures were investigated for their antiviral chemotherapeutic potency in 893 tests in cell cultures and 461 animal tests. It can be stated that compounds with a low molecular weight containing the "effective structures" (see article) show a larger yield of antiviral compounds than do substances without these structures (about 50% positive results in cell cultures and 25% in animals 15% and 0%, respectively).
D000818:Animals; D000998:Antiviral Agents / Q000494:pharmacology*; D001681:Biological Assay; D001853:Bone Marrow / Q000187:drug effects; D002467:Cell Nucleus / Q000187:drug effects; D002478:Cells, Cultured; D002869:Chromosome Aberrations; D007093:Imidazoles / Q000494:pharmacology*; D007189:Indans / Q000494:pharmacology*; D007192:Indenes / Q000494:pharmacology*; D008297:Male; D051379:Mice; D009153:Mutagens; D009154:Mutation; D009975:Orthomyxoviridae / Q000187:drug effects; D017955:Poliovirus / Q000187:drug effects; D051381:Rats; D018108:Respirovirus / Q000187:drug effects; D012229:Rhinovirus / Q000187:drug effects; D012526:Satellite Viruses / Q000187:drug effects; D018139:Simplexvirus / Q000187:drug effects; D013093:Spermatogonia / Q000187:drug effects; D013844:Thiazoles / Q000494:pharmacology*; D014616:Vaccinia virus / Q000187:drug effects
D000998:Antiviral Agents; D007093:Imidazoles; D007189:Indans; D007192:Indenes; D009153:Mutagens; D013844:Thiazoles
Experimentelle Ergebnisse mit gezielt synthetisierten Substanzen zur antiviralen Chemotherapie. 4. Der Wert hysikalischer Bindungen bei der Synthese antiviraler Chemotherapeutika und deren Einfluss auf potentielle mutagene Effekte