Studies on antiviral agents. II. Synthesis and in vitro antiviral activity on new kanamycin A derivatives having higher acyl group at N-1 position.

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Abstract
The synthesis and antiviral activity of 3''''-N-trifluoroacetylkanamycin A derivatives (6) having higher acyl group at the N-1 position are described. On the basis of the structure-activity relationships between antiviral activity and alkyl chain length in an acyl group at the N-1 position, analogs (6f .apprx. 1) having higher alkylcarbonyl group exhibited antiviral activity against not only HSV-1 but also influenza virus. Analogs (6q .apprx. v) having higher alkyloxycarbonyl group showed antiviral activity against HSV-I. In addition, kanamycin A derivatives (6n, o, y, z) possessing higher alkylcarbonyl group with a functional group, higher alkylaminocarbonyl group, and higher alkylthiocarbonyl group had antiviral activity against HSV-I. The analog (6h) showed a broad antiviral spectrum against both DNA (HSV-I, HSV-II, VZV) and RNA (influenza) viruses.