Class A GPCR-binding compound modifier
AssigneeRiken
InventorsShigeyuki Yokoyama, Tetsuya Hori
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Abstract
To provide a novel class-A GPCR antagonist, a production method therefor, or a novel compound that interacts with a Na+-water cluster binding site of a class-A GPCR. Used is a compound or a salt thereof comprising a structure comprising a class-A GPCR-binding compound linked to a functional group that can bind to a Na+-water cluster binding site of the class-A GPCR. Also used is a method for producing a class-A GPCR antagonist, comprising the step of linking one compound with another compound that can bind to a Na+-water cluster binding site of the class-A GPCR.
Claims14
A compound or a salt thereof, consisting of a structure of a class-A GPCR-binding compound linked to ring C of a functional group via a triazole linker or a triazole linker having an alkyl chain, wherein the functional group has the following structure (1):
- wherein
- ring C is a 3-to-6-membered saturated or unsaturated carbon ring group or heterocyclic group;
- R1 is amidinyl, N-hydroxyamidinyl, guanidyl, amidinyl-substituted guanidyl, ethylamino, methylamino, or NHCH3;
- R2 and R3 are the same or different and are H, methyl, halogen, hydroxyl, nitro, or N3;
- and
- m and n are the same or different and are each an integer of 0 to 11.
Dependencies are inferred from the claim text.