Synthesis and biological evaluation of 2-thiopyrimidine derivatives.
作者： Sham M. Sondhi , Rajendra N. Goyal , Anand M. Lahoti , Nirupma Singh , Rakesh Shukla
DOI: 10.1016/J.BMC.2005.02.047
关键词:
摘要: 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 compounds were fully characterized elemental analysis (CHN), FT-IR, (1)H NMR, and mass spectral data. One 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.) analgesic activity (75% 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) moderate against CDK-1 (IC(50)=5 microM). The other (5-20%), (25-75%) protein kinase (CDK-5, GSK-3) inhibitory activities (IC(50)> 10
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