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OwnerNed H. Heindel, Jeffrey D. Laskin +3inventors
InventorsNed H. Heindel, Jeffrey D. Laskin, Diane E. Heck, Christophe Guillon, Robert D. Rapp
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This invention claims the utility of two structural variants of functionalized 4-amino-3-mercapto-1,2,4-triazoles as inhibitors of nitric oxide synthase (NOS) and as inhibitors of malignant cell growth. This fundamental molecular construct operates as a heterocyclic mimic of the open-chain N-aminoarginines (or N-aminoguanidines) previously established as NOS inhibitors. A convenient bioassay method, using PAM 212 keratinocytes for detection and quantification of relative NOS inhibition potential in a series of candidate drugs, is described as is a bioassay for growth inhibition.
A method for the inhibition of nitric oxide synthase in a subject in need of such inhibition wherein is administered an effective amount of an inhibitor having the Class of either VII or X as shown below. In each class, R and R′ may constitute alkyl, aryl, hydrogen, halogen, fluoroalkyl, or heterocyclic.
A method for the inhibition of cellular proliferation in a subject in need of such inhibition wherein is administered an effective amount of an inhibitor having the Class of either VII or X as shown below. In each class, R and R′ may constitute alkyl, aryl, hydrogen, fluoroalkyl, or heterocyclic.
A method as in claim 26 to treat tuberculosis.
A method for treatment of cytotoxic or cytostatic organisms through the inhibition of nitric oxide synthase in a subject in need of such inhibition wherein is administered an effective amount of an inhibitor having the Class of either VII or X as shown below. In each class, R and R′ may constitute alkyl, aryl, hydrogen, halogen, fluoroalkyl, or heterocyclic.
Dependencies are inferred from the claim text.