Synthesis and Biological Evaluation of N-Aminoimidazolidin-2-one-Containing Angiotensin-(1–7) Peptidomimetics,Organic Letters

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Synthesis and Biological Evaluation of N-Aminoimidazolidin-2-one-Containing Angiotensin-(1–7) Peptidomimetics
Organic Letters ( IF 4.9 ) Pub Date : 2020-10-26 , DOI: 10.1021/acs.orglett.0c03070
Chuan Dai ₁ , Fang Wang ₁ , Dandan Zhang ₁ , Lei Xu ₁ , Xuefeng Xia ₁ , Jinqiang Zhang ₁

Affiliation

N-Aminoimidazolidin-2-one (Aid)-containing peptides with a constrained backbone present a novel class of peptidomimetics for drug discovery. The introduction of Aid residues into peptide sequences has been achieved by intramolecular Mitsunobu cyclization of a serine side chain onto the α-NH of an aza-glycine residue. The effectiveness of this new strategy was demonstrated by synthesizing six Aid-containing analogues of angiotensin-(1–7) on solid support. The Aid analogues of angiotensin-(1–7) exhibited increased peptidase stability against human ACE and DPP3 and improved anti-inflammation and antiproliferation activity.

中文翻译：

N-Aminoimidazolidin-2-one-Containing Angiotensin-(1–7) Peptidomimetics 的合成和生物学评价

含有N -Aminoimidazolidin-2-one (Aid) 的具有受限骨架的肽提供了一类用于药物发现的新型肽模拟物。通过丝氨酸侧链的分子内光信环化到氮杂甘氨酸残基的 α-NH 上，已实现将 Aid 残基引入肽序列。通过在固体支持物上合成六种含 Aid 的血管紧张素-(1-7) 类似物，证明了这种新策略的有效性。血管紧张素-(1-7) 的 Aid 类似物表现出对人 ACE 和 DPP3 的肽酶稳定性增加，并改善了抗炎和抗增殖活性。

更新日期：2020-11-06

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