Author/Authors :
David T. Hill، نويسنده , , Gerald R. Girard، نويسنده , , Joseph Weinstock، نويسنده , , Richard M. Edwards، نويسنده , , Edwin F. Weidley، نويسنده , , Eliot Ohlstein، نويسنده , , Catherine E. Peishoff، نويسنده , , Elayne Baker، نويسنده , , Nambi Aiyar، نويسنده ,
Abstract :
A series of D and L-N-[(1-benzyl-1H-imidazol-5-yl)-alkyl]-aromatic amino acids (2 to 9) and several achiral analogs (1,10,11) were found to be potent AII antagonists (nM range). Among chiral pairs the D isomer had the highest affinity for the binding site. A D-phenylalanine analog, 3, was the most potent (IC50 3.8 nM) and had activity in vivo similar to SK&F 108566 when given i.v. but was only marginally active when given i.d.
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