Kim Youngjae, Kim Minjoo, Park Mooseong, Tae Jinsung, Baek Du-Jong, Park Ki Duk, Choo Hyunah
Center for Neuro-Medicine, Korea Institute of Science and Technology, Seongbuk-gu, Seoul 136-791, Korea.
Department of Chemistry, Yonsei University, Seodaemun-gu, Seoul 120-749, Korea.
Molecules. 2015 Mar 19;20(3):5074-84. doi: 10.3390/molecules20035074.
A novel molecular scaffold, dihydropyridothienopyrimidin-4,9-dione, was synthesized from benzylamine or p-methoxybenzylamine in six steps involving successive ring closure to form a fused ring system composed of dihydropyridone, thiophene and pyrimidone. The pharmacological versatility of the dihydropyridothenopyrimidin-4,9-dione scaffold was demonstrated by inhibitory activity against metabotropic glutamate receptor subtype 1 (mGluR1), which shows that the title compounds can serve as an interesting scaffold for the discovery of potential bioactive molecules for the treatment of human diseases.
一种新型分子骨架二氢吡啶并噻吩并嘧啶 -4,9- 二酮，由苄胺或对甲氧基苄胺经六步合成，包括连续闭环以形成由二氢吡啶酮、噻吩和嘧啶酮组成的稠环体系。二氢吡啶并噻吩并嘧啶 -4,9- 二酮骨架的药理多功能性通过对代谢型谷氨酸受体亚型 1（mGluR1）的抑制活性得到证明，这表明标题化合物可作为发现治疗人类疾病潜在生物活性分子的有趣骨架。
