Synthesis and pharmacological evaluation of several ring-contracted amantadine analogs.
Synthesis and pharmacological evaluation of several ring-contracted amantadine analogs.
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DOI：
10.1016/j.bmc.2008.10.028
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发表时间：
2008-12-01
影响因子：
3.5
通讯作者：
Cortés D
中科院分区：
文献类型：
--
作者：
Camps P;Duque MD;Vázquez S;Naesens L;De Clercq E;Sureda FX;López-Querol M;Camins A;Pallàs M;Prathalingam SR;Kelly JM;Romero V;Ivorra D;Cortés D
合成了几个双去甲烷胺和去甲烷胺，并研究了它们的抗病毒、杀锥虫、NMDA受体拮抗剂和多巴胺再摄取抑制活性。报道了几种(3-去甲金刚烷基)胺、[(3-去甲金刚烷基)甲基]胺、(3，7-二甲基-1-双去甲金刚胺)胺和[(3，7-dimethyl-1-bisnoradamantyl)methyl]amines的合成。对多种病毒进行了评估，其中一种药物在与金刚烷胺相似的浓度下抑制了甲型流感病毒的细胞病变。一些新的多环胺类化合物显示出作为NMDA受体拮抗剂的有趣的活性。金刚乙胺类似物显示出显著的杀锥虫活性。此外，为了进一步确定这些化合物的药理作用，还评估了它们对多巴胺摄取的影响。
Several bisnoradamantylamines and noradamantylamines have been synthesized and their antiviral, trypanocidal, NMDA receptor antagonist, and dopamine reuptake inhibitory activities have been studied. The synthesis of several (3-noradamantyl)amines, [(3-noradamantyl)methyl]amines, (3,7-dimethyl-1-bisnoradamantyl)amines, and [(3,7-dimethyl-1-bisnoradamantyl)methyl]amines is reported. They were evaluated against a wide range of viruses and one of them inhibited the cytopathicity of influenza A virus at a concentration similar to that of amantadine. Several of the new polycyclic amines show an interesting activity as NMDA receptor antagonists. A rimantadine analogue displayed significant trypanocidal activity. Moreover, to further characterize the pharmacology of these compounds, their effects on dopamine uptake were also assessed.
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影响因子：
7.6
作者：
Burstein, ME;Serbin, AV;Bukrinskaya, AG
通讯作者：
Bukrinskaya, AG
影响因子：
2.1
作者：
Camps, P;Lukach, AE;Vázquez, S
通讯作者：
Vázquez, S
影响因子：
3.5
作者：
Geldenhuys, Werner J.;Malan, Sarel F.;Van der Schvf, Cornelis J.
通讯作者：
Van der Schvf, Cornelis J.
DOI：
10.1038/nrd2175
发表时间：
2006-12
期刊：
Nature reviews. Drug discovery
影响因子：
--
作者：
De Clercq E
通讯作者：
De Clercq E
影响因子：
3.6
作者：
Ayats, C;Camps, P;Vázquez, S
通讯作者：
Vázquez, S