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ID: ALA1131934

Journal: Bioorg Med Chem Lett

Title: The design of non-peptide human bradykinin B2 receptor antagonists employing the benzodiazepine peptidomimetic scaffold.

Authors: Dziadulewicz EK, Brown MC, Dunstan AR, Lee W, Said NB, Garratt PJ.

Abstract: 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 microM at the human Bradykinin B2 receptor.

CiteXplore: 10091703

DOI: 10.1016/s0960-894x(99)00015-3