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目的利用骨架跃迁思想设计并合成新型水杨酰苯胺类代谢型谷氨酸受体5(metabotropic glutamate receptor5,mglu5)拮抗剂。方法将取代水杨酸与二取代苯胺缩合得目标化合物Ⅰ-Ⅳ,用核磁共振和质谱进行结构确证,荧光测钙流法进行拮抗mglu5活性测定。结果设计的目标化合物对mglu5具有明显的拮抗活性,其中化合物Ⅰ拮抗活性最好,IC_(50)为0.079μmol/L。结论水杨酰苯胺类化合物为潜在的新型mglu5拮抗剂,值得进一步研究。
OBJECTIVE: To design and synthesize a novel metabotropic glutamate receptor 5 (mglu5) antagonist by using the skeleton transition thought. Methods The target compounds Ⅰ-Ⅳ were obtained by condensation of substituted salicylic acid with di-substituted anilines. The structures were confirmed by 1H NMR and MS spectra. The antagonistic activity of mglu5 was determined by fluorimetric calcium current method. Results The designed target compounds showed obvious antagonistic activity against mglu5, of which compound Ⅰ showed the best antagonistic activity with IC 50 of 0.079 μmol / L. Conclusions Salicylanilide is a new potential antagonist of mglu5 and deserves further study.