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一类新型钠/钙交换抑制剂：4-苯基-3-(哌啶-4-基)-3,4-二氢-2(1H)-喹唑啉酮衍生物的设计、合成及构效关系

A novel class of sodium/calcium exchanger inhibitors: design, synthesis, and structure-activity relationships of 4-phenyl-3-(piperidin-4-yl)-3,4-dihydro-2(1H)-quinazolinone derivatives.

作者信息

Hasegawa Hirohiko, Muraoka Masami, Matsui Kazuki, Kojima Atsuyuki

机构信息

Research Division, Sumitomo Pharmaceuticals Co. Ltd, 1-98, Kasugadenaka 3-Chome, Konohana-ku, Osaka 554-0022, Japan.

出版信息

Bioorg Med Chem Lett. 2006 Feb;16(3):727-30. doi: 10.1016/j.bmcl.2005.10.012. Epub 2005 Oct 24.

DOI:10.1016/j.bmcl.2005.10.012
PMID:16249082
Abstract

Design, synthesis, and structure-activity relationships of 3,4-dihydro-2(1H)-quinazolinone derivatives as sodium/calcium (Na+/Ca2+) exchanger inhibitors are described. In these studies, optimization of the substituents at the 3-position of this series of compounds was carried out and dramatic effects of the substituent on the activities were observed. Based on these SAR studies, a highly potent inhibitor of the Na+/Ca2+ exchanger, which showed single-digit-nanomolar activity, was discovered.

摘要

描述了作为钠/钙（Na+/Ca2+）交换抑制剂的3,4-二氢-2(1H)-喹唑啉酮衍生物的设计、合成及构效关系。在这些研究中，对该系列化合物3位的取代基进行了优化，并观察到取代基对活性有显著影响。基于这些构效关系研究，发现了一种高效的Na+/Ca2+交换抑制剂，其活性达到个位数纳摩尔级别。

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