LCZ696: a dual-acting sodium supramolecular complex

被引:91
作者
Feng, Lili [1 ]
Karpinski, Piotr H. [1 ]
Sutton, Paul [1 ]
Liu, Yugang [1 ]
Hook, David F. [2 ]
Hu, Bin [1 ]
Blacklock, Thomas J. [1 ]
Fanwick, Philip E. [3 ]
Prashad, Mahavir [1 ]
Godtfredsen, Sven [1 ]
Ziltener, Christoph [2 ]
机构
[1] Novartis Pharmaceut, E Hanover, NJ 07936 USA
[2] Novartis Pharma AG, CH-4056 Basel, Switzerland
[3] Purdue Univ, Dept Chem, W Lafayette, IN 47907 USA
关键词
LCZ696; Hypertension; X-ray crystallography; ARNI; Supramolecular complex; INHIBITOR; RECEPTOR; NEPRILYSIN;
D O I
10.1016/j.tetlet.2011.11.029
中图分类号
O62 [有机化学];
学科分类号
070303 [有机化学];
摘要
LCZ696 displays several surprising features, such as an intrinsic stabilization of the supramolecular complex by monovalent multi-coordinated sodium cations and water molecules. In addition, to the best of our knowledge, the compound is the first example of a dual-acting pharmaceutical built as a supramolecular complex delivering two pharmacologic effects angiotensin receptor 1 (AT1) blockage and neprilysin (NEP) inhibition. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码:275 / 276
页数:2
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