新型酮基-ACE类似物作为结构域选择性血管紧张素I转换酶抑制剂的合成
Synthesis of novel keto-ACE analogues as domain-selective angiotensin I-converting enzyme inhibitors.
作者信息
Nchinda Aloysius T, Chibale Kelly, Redelinghuys Pierre, Sturrock Edward D
机构信息
Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Observatory 7925, South Africa.
出版信息
Bioorg Med Chem Lett. 2006 Sep 1;16(17):4612-5. doi: 10.1016/j.bmcl.2006.06.003. Epub 2006 Jun 19.
PMID:16784850
Abstract
Novel analogues of the angiotensin I-converting enzyme (ACE) inhibitor keto-ACE were synthesized via a facile Horner-Emmons olefination of a phosphonoketone precursor with ethyl glyoxylate. Introduction of a bulky aromatic tryptophan at the P(2)(') position of keto-ACE resulted in a significant increase in C-domain-selectivity.
摘要
通过膦酰基酮前体与乙醛酸乙酯的简便霍纳-埃蒙斯烯烃化反应，合成了血管紧张素I转换酶（ACE）抑制剂酮-ACE的新型类似物。在酮-ACE的P(2)' 位引入一个庞大的芳香族色氨酸，导致C结构域选择性显著增加。
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