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(2-氧杂金刚烷-1-基)胺的合成与药理评价

Synthesis and pharmacological evaluation of (2-oxaadamant-1-yl)amines.

作者信息

Duque María D, Camps Pelayo, Profire Lenuta, Montaner Silvia, Vázquez Santiago, Sureda Francesc X, Mallol Jordi, López-Querol Marta, Naesens Lieve, De Clercq Erik, Prathalingam S Radhika, Kelly John M

机构信息

Laboratori de Química Farmacèutica (Unitat Associada al CSIC), Facultat de Farmàcia, and Institute of Biomedicine (IBUB), Universitat de Barcelona, Av. Diagonal, 643, Barcelona E-08028, Spain.

出版信息

Bioorg Med Chem. 2009 Apr 15;17(8):3198-206. doi: 10.1016/j.bmc.2009.02.007. Epub 2009 Feb 13.

Abstract

The synthesis of several (2-oxaadamant-1-yl)amines is reported. They were evaluated as NMDA receptor antagonists and several of them were more active than amantadine, but none was more potent than memantine. None of the tested compounds displayed antiviral activity. Two of the derivatives showed a significant level of trypanocidal activity.

摘要

报道了几种(2-氧杂金刚烷-1-基)胺的合成。它们被评估为NMDA受体拮抗剂,其中几种比金刚烷胺更具活性,但没有一种比美金刚更有效。所测试的化合物均未显示出抗病毒活性。其中两种衍生物表现出显著水平的杀锥虫活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/876b/7127296/fd0d404c7c66/fx1.jpg

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