membrane-permeable neuraminidase inhibitor

schaub at chclu.chemie.uni-konstanz.de schaub at chclu.chemie.uni-konstanz.de
Wed Apr 23 08:03:01 EST 1997


In article <l03010d03af825238039f@[194.94.45.100]>, Derek.Toomre at EMBL-HEIDELBERG.DE (Derek Toomre) writes:
>Please...Could anyone tell me if they know of a membrane permeable
>neuramidase inhibitor?
>
>I know that potent 4-guanidino-Nue5Ac2en analogues exist, but are these or
>other inhibitors able to penetrate the membrane barrier?
>
>Specifically I would like to block the sialidase activity of influenza A
>infected MDCK cells so that the HA which is sent out to the PM remains
>sialylated?
>
>Thanks for any help.
>
>-Derek
>
>-=-=-=-=-=-=-=-=-=-=-=-=-=-=-=-=-=-=-=-=-=-=-=-=-=-=-
Hello Derek,

recently (I think in january) there was published a new sialidase inhibtor in
JACS (Kim et al., JACS, 1997, 119, 681-9)which should be more lipophilic and for that reason probaly membran
permeable. The inhibition values are as good as those of the Itzstein inhibitor
but the synthesis is rather long. Probably you can contact those people to get
the substance

Christoph

--------------------------------
Christoph Schaub
Fakultaet fuer Chemie
Universitaet Konstanz
Germany



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