设计、合成并评价含黄酮片段的新型芳基哌嗪衍生物作为α1-肾上腺素能受体拮抗剂。
Design, synthesis and biological evaluation of new arylpiperazine derivatives bearing a flavone moiety as α1-adrenoceptor antagonists.
机构信息
Department of Natural Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People's Republic of China.
出版信息
Bioorg Med Chem Lett. 2011 Feb 1;21(3):909-11. doi: 10.1016/j.bmcl.2010.12.080. Epub 2010 Dec 21.
PMID:21236664
Abstract
Elaborate study on the three-dimensional model of α(1)-adrenoceptor (α(1)-AR) antagonists led to the development of a series of new arylpiperazine derivatives bearing a flavone nucleus as α(1)-AR antagonists. The in vitro activities were evaluated and compounds 1, 4, 10, 13 and 15 showed activities close to the reference compound (Prazosin).
摘要
对 α(1)-肾上腺素受体（α(1)-AR）拮抗剂的三维模型进行深入研究，开发了一系列新型芳基哌嗪衍生物，其具有黄酮核作为 α(1)-AR 拮抗剂。评估了它们的体外活性，化合物 1、4、10、13 和 15 表现出与参比化合物（哌唑嗪）相近的活性。
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