Lijun Zhang, Matthew A. Williams, Dirk B. Mendel, Paul A. Escarpe, Xiaowu Chen, Ke-Yu Wang, Bradford J. Graves, Geoff Lawton, Choung U. Kim
Synthesis and Evaluation of 1,4,5,6-Tetrahydropyridazine Derivatives as Influenza Neuraminidase Inhibitors.-The highly functionalized title derivatives (VI) and (IX) are rapidly synthesized via a hetero Diels-Alder reaction. A µM range of influenza neuraminidase inhibitory activity is shown by these derivatives. This low activity is consistent with the results from X-ray crystallography and NMR studies. Significantly increased activity is obtained by converting the amino group of (VI) into a guanidino functio…
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