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Synthesis and evaluation of 1,4,5,6-tetrahydropyridazine derivatives as influenza neuraminidase inhibitors

1999; Elsevier BV; Volume: 9; Issue: 13 Linguagem: Inglês

10.1016/s0960-894x(99)00280-2

1464-3405

Lijun Zhang, Matthew A. Williams, Dirk B. Mendel, Paul A. Escarpe, Xiaowu Chen, Keyu Wang, Bradford Graves, Geoff Lawton, Choung U. Kim,

Click Chemistry and Applications

1,4,5,6-Tetrahydropyridazine derivative 15 and its C-5 epimer 19, which possessed side chains similar to GS4071, were synthesized via a hetero Diels-Alder reaction, and evaluated as influenza neuraminidase inhibitors. Compounds 15 and 19 exhibited a μM range of influenza neuraminidase inhibitory activity.