Renal-selective compounds are described which, in one embodiment, are
prodrugs preferentially converted in the kidney to compounds capable of
blocking angiotensin II (AII) receptors. These prodrugs are conjugates
formed from two components, namely, a first component provided by an AII
antagonist compound and a second component which is capable of being
cleaved from the first component when both components are chemically
linked within the conjugate. The two components are chemically linked by
a bond which is cleaved selectively in the kidney, for example, by an
enzyme. The liberated AII antagonist compound is then available to block
AII receptors within the kidney. Conjugates of particular interest are
glutamyl derivatives of biphenylmethyl 1H-substituted-1,2,4-triazole
compounds, of which N-acetylglutamic acid,
5-[[4'-[(3,5-dibutyl-1H-1,2,4-triazol-1-yl)methyl][1,1'-biphenyl]-2-yl]]c-
arbonylhydrazide, (shown below) is an example: ##STR00001##