SYNTHESIS AND PHARMACOLOGICAL ACTIVITIES OF SOME 3-SUBSTITUTED THIENOPYRIMIDIN-4-ONE-2-THIONES

The condensation of substituted 2-amino-3-carbethoxy-thiophenes with methyl, ethyl and phenyl isothiocyanate yields the corresponding thienylthioureas which cyclize in ethanol saturated with dry hydrochloric acid to form 3-substituted thieno [2,3-d]pyrimidin-4-(3H)-one-2-thiones. Thirty-five compounds, 21 thienylthioureas and 14 thienopyrimidin-4-one-2-thiones have been screened for their analgesic and anti-inflammatory activities. The ip administration of these products at a dose of 1000 mg/kg shows that they are not toxic (one excepted). Some compounds show analgesic and anti-inflammatory activities equivalent to those of acetylsalicylic acid. © 1990.