The design of non-peptide human bradykinin B2 receptor antagonists employing the benzodiazepine peptidomimetic scaffold |
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| Authors: | Dziadulewicz E K Brown M C Dunstan A R Lee W Said N B Garratt P J |
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| Affiliation: | Novartis Institute for Medical Sciences, London, UK. ed.dziadulewicz@pharma.novartis.com |
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| 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. |
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