Thiazoline ring compounds as botulinum antagonists
AssigneeBioMadison, Inc.
InventorsFüsûn N. Zeytin, Ward Tucker
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Abstract
Compositions and methods for inhibiting BoNT protease activity are presented. In most preferred aspects, inhibitors comprise a thiol reactive group, a zinc binding group, a redox active group, an alkylating group, and/or an electrophilic Michael addition acceptor group. Particularly preferred inhibitors include an isothiazolone ring, a thiadiazolidine dione ring, a (hydro)quinone ring, an iminophenol group, and/or a hydrazonophenol group, and inhibit BoNT/A at μM and sub-μM concentrations.
Claims3
A method of inhibiting BoNT-A light chain activity comprising a step of contacting the BoNT-A light chain with a compound having a structure according to Formula 1:
- wherein Y is S;
- R2 is ═O;
- R1 is an optionally substituted alkyl or aryl;
- R3, and R4 are independently H, alkyl, alkenyl, alkaryl, aryl, heteroalkyl, or heteroaryl, wherein each of R3 and R4 may be optionally substituted with one or more substituents, wherein R3 and R4 may optionally form a ring, which may be a heterocyclic ring, and wherein the heterocyclic ring that includes N and Y in Formula I optionally has one or more double bonds.
Dependencies are inferred from the claim text.