ABSTRACT
The synthesis of various substituted nitroimidazoles with lipophilic and hydrophilic side chains as potential radiosensitizing agents is described. The starting material employed was 4(5)-nitroimidazole, which was alkylated via the sodium salt with various chloro-methylated, substituted alcohols and esters, in order to obtain analogues of misonidazole, metronidazole and desmethylmisonidazole of known radiosensitizing and bactericidal activity. Some final products were assayed for their radiosensitizing properties giving negative results under the testing conditions used.
Subject(s)
Nitroimidazoles/chemical synthesis , Radiation-Sensitizing Agents/chemical synthesis , In Vitro Techniques , Molecular Structure , Nitroimidazoles/pharmacology , Radiation Tolerance/drug effects , Radiation-Sensitizing Agents/pharmacology , Structure-Activity Relationship , Tumor Cells, Cultured/drug effectsABSTRACT
The synthesis of 1-substituted, acyclic nucleoside derivatives of 5(6)-nitrobenzimidazoles and their pharmacological evaluation as antiviral compounds is described. The compounds were synthesized using 5(6)-benzimidazole as starting material with the appropriate chloromethylated substituted alcohols to obtain analogues of the known antiviral compounds, Acyclovir and Ganciclovir. The antiviral activity of these compounds was evaluated using strains of Herpes Simplex 1 and Poliovirus 1 and were found to be inactive as antiviral compounds under the testing conditions employed.