Moutevelis-Minakakis P, Gianni M, Stougiannou H, Zoumpoulakis P, Zoga A, Vlahakos A D, Iliodromitis E, Mavromoustakos T
University of Athens, Department of Chemistry, Zographou 15771, Greece.
Bioorg Med Chem Lett. 2003 May 19;13(10):1737-40. doi: 10.1016/s0960-894x(03)00251-8.
AT1 antagonists constitute a new generation of drugs for the treatment of hypertension and are designed and synthesized to mimic the C-terminal segment of Angiotensin II (Ang II) and to block its binding action on AT1 receptor. For this reason, the conformational analysis of Ang II and its derivatives as well as the AT1 antagonists belonging to SARTANs class of molecules were studied. Such studies offer the possibility to reveal the stereoelectronic factors responsible for bioactivity of AT1 antagonists and to design and synthesize new analogues with better pharmacological and financial profiles. An example of a novel synthetic non-peptide molecule is given which mimics the His(6)-Pro(7)-Phe(8) part of Ang II and is based on the (S)-pyroglutamic acid.
AT1拮抗剂是治疗高血压的新一代药物，其设计和合成旨在模拟血管紧张素II（Ang II）的C末端片段，并阻断其对AT1受体的结合作用。因此，对Ang II及其衍生物以及属于SARTANs类分子的AT1拮抗剂进行了构象分析。此类研究为揭示负责AT1拮抗剂生物活性的立体电子因素以及设计和合成具有更好药理和经济特性的新类似物提供了可能性。给出了一个新型合成非肽分子的实例，该分子模拟了Ang II的His(6)-Pro(7)-Phe(8)部分，并基于（S）-焦谷氨酸。
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