Santagati N A, Caruso A, Cutuli V M, Caccamo F
Instituto di Chimica Farmaceutica e Tossicologica, Università di Catania, Italy.
Farmaco. 1995 Oct;50(10):689-95.
Two series of novel derivatives based on the thienopyrimidine and pyrimidoindole ring systems, both N-substituted in position 3, have been synthesized. The compounds were obtained by reaction of N-amino groups of 5,6-dimethyl-thieno[2,3-d]pyrimidin-2,4-dione and of 5H-pyrimido[5,4-b]indol-2,4-dione with aromatic aldehydes. Some of these substances showed an appreciable analgesic activity, a good antiinflammatory activity, a low acute toxicity with an optimal gastric tolerance.
已经合成了基于噻吩并嘧啶和嘧啶并吲哚环系的两个系列的新型衍生物，两者均在3位进行了N-取代。这些化合物是通过5,6-二甲基-噻吩并[2,3-d]嘧啶-2,4-二酮和5H-嘧啶并[5,4-b]吲哚-2,4-二酮的N-氨基与芳香醛反应得到的。其中一些物质表现出明显的镇痛活性、良好的抗炎活性、低急性毒性以及最佳的胃耐受性。
