160133-75-5Relevant articles and documents
Synthesis and biological evaluation of N3-alkyl-thienopyrimidin-4-ones as mGluR1 antagonists
Kim, Minjoo,Kim, Youngjae,Seo, Seon Hee,Baek, Du-Jong,Min, Sun-Joon,Keum, Gyochang,Choo, Hyunah
, p. 1439 - 1451 (2015/07/15)
Metabotropic glutamate receptor subtype 1 (mGluR1) is a potential target for the treatment of neuropathic pain, and there has been much effort to discover mGluR1 antagonists. In this study, a series of N3-alkyl-thienopyrimidin-4-ones were prepared by introducing various alkyl and aryl groups to the N3- and 7-positions of the thienopyrimidin-4-one core structure, respectively, and their inhibitory activities against mGluR1 were biologically evaluated. Structure-activity relationship study revealed that the trans-4-methylcyclohexyl, cycloheptyl, and cyclooctyl groups at N3-position, and 2-fluorophenyl group at 7-position were most effective in potentiating the inhibitory activity of the thienopyrimidin-4-one derivatives against mGluR1. Among the synthesized compounds, 3-cyclooctyl-7-phenylthienopyrimidin-4-one and 3-cycloheptyl-7-(2-fluorophenyl)thienopyrimidin-4-one exhibited the most potent inhibitory activities with IC50 values of 115 and 107 nM, respectively.
Synthesis of thieno[3,2-d]pyrimidine-2,4-diones cyclic and acyclic nucleosides as potential anti HIV agents
Jourdan,Laduree,Robba
, p. 305 - 312 (2007/10/02)
Synthesis of cyclic and acyclic nucleosides was achieved by alkylation of 7-methyl or arylthieno[3,2-d]pyrimidine-2,4-diones following the Vorbruggen and Niedballa's method [1]. After a possible deprotection, potential anti HIV agents were obtained.