The design and synthesis of a series of 2-(3-indolylmethyl)-4-(tert-butoxyc
arbonyl)-1,4-diaza-2-oxobicyclo [4.3.0]nonane-9-carboxylic acid peptidomime
tics based on the peptide endothelin antagonists BQ-123 and FR139317 were d
escribed. The stereochemistry of the active (3R,6S,9R) isomer was determine
d by X-Ray crystallography.