The design of non-peptide human bradykinin B2 receptor antagonists employing the benzodiazepine peptidomimetic scaffold.
作者： Edward K. Dziadulewicz , Michael C. Brown , Andrew R. Dunstan , Wai Lee , Najeeb B. Said
DOI: 10.1016/S0960-894X(99)00015-3
关键词: Antagonist 、 Receptor 、 Bradykinin 、 Biological activity 、 Chemistry 、 Bradykinin receptor 、 Bradykinin B2 Receptor Antagonists 、 Chemical synthesis 、 Peptidomimetic 、 Stereochemistry
摘要: 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 small number non-peptide lead compounds based on 1,4-benzodiazepin-2-one framework. Two have found to exhibit moderate K(i) values 8.9 9.2 microM at human receptor.
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