The design of non-peptide human Bradykinin B2 receptor antagonists employing the benzodiazepine peptidomimetic scaffold

Article abstract of DOI:10.1016/S0960-894X(99)00015-3

The Bradykinin B₂ receptor antagonist HOE 140 (D-Arg-Arg-Pro-Hyp-Gly- Thi-Ser-D-Tic-Oic-Arg) has been used as a template for the de novo design and synthesis of a small number of non-peptide lead compounds based on the 1,4- benzodiazepin-2-one framework. Two of the compounds have been found to exhibit moderate K(i) values of 8.9 and 9.2 μM at the human Bradykinin B₂ receptor.