کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1394470 | 1501158 | 2012 | 10 صفحه PDF | دانلود رایگان |
The synthesis in 4 steps of new N,N′-bis(5-arylidene-4-oxo-3,5-dihydro-4H-imidazol-2-yl)diamines issued from various symmetric primary diamines as linkers was reported. The key step of our strategy has been the sulphur/nitrogen displacement of (5Z)-5-arylidene-2-ethylsulfanyl-3,5-dihydro-4H-imidazol-4-ones 6 with respectively ethylenediamine 7a, piperazine 7b and N,N′-bis(3-aminopropyl)piperazine 7c using solvent-free reaction conditions under microwave irradiation with retention of configuration. These compounds were tested for their kinase inhibitory potencies toward four kinases (GSK-3α/β, DYRK1A, CLK1 and CLK3).
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► A new route N,N′-bis(5-arylidene-4-oxo-3,5-dihydro-4H-imidazol-2-yl)diamines.
► N,N′-disubstituted diamines with3 points of diversity.
► Sulphur/nitrogen displacement under solvent-less microwave irradiation reaction conditions.
► Inhibitor of the CLK1 kinase.
Journal: European Journal of Medicinal Chemistry - Volume 58, December 2012, Pages 581–590