Thiol-based NAALADase inhibitors

Abstract

This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-β activity, inhibiting angiogenesis and treating glutamate abnormalities, diabetic neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.

1 . A compound of formula I  
     
       
         
         
             
             
         
       
     
     or a pharmaceutically acceptable equivalent of said compound, wherein: 
 R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7  and R 8  are independently hydrogen or C 1 -C 3  alkyl;  
 A 1 , A 2 , A 3  and A 4  are independently hydrogen, C 1 -C 6  alkyl, C 1 -C 6  alkoxy, halo, nitro, phenyl, phenoxy, benzyloxy or —COOH, or any adjacent two of A 2 , A 3  and A 4  form with the benzene ring a fused 5- or 6-membered carbocyclic or heterocyclic aromatic ring, said heterocyclic aromatic ring containing 1 or 2 oxygen, nitrogen and/or sulfur heteroatom(s).