کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1364203 | 981531 | 2005 | 11 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Synthesis and biological evaluation of 2-thiopyrimidine derivatives Synthesis and biological evaluation of 2-thiopyrimidine derivatives](/preview/png/1364203.png)
Various 2-thiopyrimidine derivatives have been synthesized by an efficient, one-pot reaction of functionalized amines with either 4-isothiocyanato-4-methyl-2-pentanone or 3-isothiocyanatobutanal. All the synthesized compounds were fully characterized by elemental analysis (CHN), FT-IR, 1H NMR, and mass spectral data. One of the compounds, 7,7,8a-trimethyl-hexahydro-thiazolo[3,2-c]pyrimidine-5-thione (17) showed good anti-inflammatory (37.4% at 100 mg/kg p.o.) and analgesic activity (75% at 100 mg/kg p.o.). 7-(1-Mercapto-3,3,4a-trimethyl-4,4a,5,9b-tetrahydro-3H-pyrido[4,3-b]indol-7-yl)-3,3,4a-trimethyl-3,4,4a,5-tetrahydro-benzo[4,5]imidazo[1,2-c]pyrimidine-1-thiol (3) showed moderate activity against CDK-1 (IC50 = 5 μM). The other compounds showed moderate anti-inflammatory (5–20%), analgesic (25–75%) and protein kinase (CDK-5, GSK-3) inhibitory activities (IC50 > 10 μM).
Various 2-thiopyrimidine derivatives have been synthesized by condensation of functionalized amines with β-isothiocyanatoketones. Some compounds showed moderate to good activities for anti-inflammatory, analgesic, and protein kinase (CDK-1) inhibition.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry - Volume 13, Issue 9, 2 May 2005, Pages 3185–3195