Synthesis of N-thiocarbamoyl derivatives of N-amino nucleic acid bases and their antiviral activity

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(1) We have previously synthesized a new class of nucleic acid base analogs, "N-amino nucleic acid bases". In the present study, these N-amino compounds were converted to N-thiocarbamoyl derivatives, which are expected to be a new class of antiviral agents. A general formula is given as (aromatic) N-NH-CS-NRR', where R and R' are H,methyl, ethyl, or propyl group. The biological activities including antiviral activity are under investigation.(2) In order to develop a new class of alkylating N-nitrosoureas, N-amino nucleic acid bases were converted to N-carbamoyl derivatives, followed by N-nitrosation to afford a new class of alkylating N-nitroso analogs, which are expected to a new class of anticancer agents. These N-aminonitrosourea analogs are distinguished from normal N-alkyl-N-nitrosoureas by pH-independent hydrolysis resulting in lethal alkylations of biomaterials. This property has the advantage of treatment of the inside of tumor tissues where pH is lower that that in the normal organ tissues. The present study provided details on the synthetic procedures and chemical characteristics of this type of N-amino-N-nitrosourea analogs and their biological activities including anticancer activity are under investigation.