The main focus of the dissertation is the synthesis of neuraminidase inhibitors. Besides
the synthesis of novel series of zanamivir derived neuraminidase inhibitors synthesis of prodrugs
of zanamivir was also presented. The synthesized prodrugs of zanamivir include gly-gln
dipeptide coupled at C-9 position of zanamivir (19), C-1 esterified zanamivir with methionine
coupled at C-9 position (23) and zanamivir esterified at C-1 position with methionine coupled 4-
aminobenzyl alcohol trigger (27). These prodrugs of zanamivir are submitted for enzyme based
biological assay to study their oral uptake efficacy.
Further, a series of C-4 modified zanamivir derivatives bearing the triazole moiety linked
to the guanidine functionality with alkyl spacer were also synthesized. The hydrolysis of the
triazole derivatives to obtain the fully deprotected products, which were intended to submit for
their biological evaluation, resulted in the cleavage of amide bond linking the guanidine group of
zanamivir and alkyl spacer with triazole.

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