Cathepsin L inhibitors and probes comprising vinyl sulfonate moiety and methods of using same
AssigneeResearch Foundation of the City University of New York
InventorsSanjai Kumar, Dibyendu Dana
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Abstract
Human cathepsin L inhibitors and probes containing a vinyl sulfonate ester moiety are described. The inhibitors are highly potent (low nM affinity), selective, and cell permeable, and can inhibit ultra-low concentration of active cathepsin L. The developed probes are highly sensitive and can detect an ultra-low amount of probe-labeled active cathespin L.
Claims20
A method for inhibiting cathepsin L or probing the activity of cathepsin L, the method comprising steps of:
- exposing a biological cell to a compound of Formula (A) or a pharmaceutically acceptable solvate, hydrate, salt or N-oxide thereof:
- wherein,
- R1 is selected from the group consisting of Br, Cl, I, an aryl, CO2CH3, CN and NO2;
- each R2 is independently selected from the group consisting of F, CF3, aryl and methyl;
- each R3 is independently selected from the group consisting of F, CF3 aryl and methyl;
- R4 is selected from the group consisting of H, CCH and N3;
- R5 is selected from the group consisting of methyl, ethyl and propyl;
- R6 is an aryl;
- n is 0, 1 or 2
- m is 0, 1 or 2.
A composition of matter with a structure given by Formula (A) or a pharmaceutically acceptable solvate, hydrate, salt or N-oxide thereof
- wherein,
- R1 is selected from the group consisting of Br, Cl, I, an aryl, CO2CH3, CN and NO2;
- each R2 is independently selected from the group consisting of F, CF3, aryl and methyl;
- each R3 is independently selected from the group consisting of F, CF3 aryl and methyl;
- R4 is selected from the group consisting of H, CCH and N3;
- R5 is selected from the group consisting of methyl, ethyl and propyl;
- R6 is an aryl;
- n is 0, 1 or 2
- m is 0, 1 or 2.
Dependencies are inferred from the claim text.