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1,8,11,11-四甲基-4-氮杂三环[5.2.2.0(2,6)]十一碳-8-烯-3,5-二酮衍生物的合成与药理活性。[已校正]

Synthesis and pharmacological activity of 1,8,11,11-tetramethyl-4-azatricyclo[5.2.2.0(2,6)]undec-8-ene-3,5-dione derivatives. [corrected].

作者信息

Pakosińska-Parys Magdalena, Kossakowski Jerzy, Mirosław Barbara, Kozioł Anna E, Stefańska Joanna

机构信息

Department of Medical Chemistry, Medical University of Warsaw, Oczki 3, 02-007 Warszawa, Poland.

出版信息

Acta Pol Pharm. 2013 May-Jun;70(3):505-15.

Abstract

The synthesis and pharmacological activity of N-substituted derivatives of 1,8,11,11-tetramethyl-4-azatricyclo[5.2.2.0(2,6)]undec-8-ene-3,5-dione (1) are described. The molecular structure of starting compound (1) was confirmed by elemental analysis, 13C NMR and X-ray crystallography. The structures of derivatives were confirmed by 1H NMR and mass spectra. The compounds were investigated for antibacterial activity, including Gram-positive cocci, Gram-negative rods, and antifungal activity. Studied compounds were evaluated also for their cytotoxicity and anti-HIV-1 activity in MT-4 cells.

摘要

描述了1,8,11,11-四甲基-4-氮杂三环[5.2.2.0(2,6)]十一碳-8-烯-3,5-二酮(1)的N-取代衍生物的合成及药理活性。起始化合物(1)的分子结构通过元素分析、13C NMR和X射线晶体学得以确证。衍生物的结构通过1H NMR和质谱得以确证。对这些化合物进行了抗菌活性研究,包括革兰氏阳性球菌、革兰氏阴性杆菌,以及抗真菌活性研究。还对所研究的化合物在MT-4细胞中的细胞毒性和抗HIV-1活性进行了评估。

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