首页|新型咪唑[1,2-a]-吡啶衍生物的设计合成及抗肺纤维化活性评价

新型咪唑[1,2-a]-吡啶衍生物的设计合成及抗肺纤维化活性评价

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咪唑[1,2-a]-吡啶是多种药物保持活性的重要母核.基于咪唑[1,2-a]-吡啶衍生化开发的ATX抑制剂可用于肺纤维化疾病治疗.以咪唑[1,2-a]-吡啶为母核,6-位及3-位胺基为修饰位点,合成了一系列新型咪唑[1,2-a]-吡啶衍生物(5a~5e,8),其结构经1H NMR、13C NMR和MS(ESI)表征.通过采用小鼠胚胎成纤维细胞(NIH/3T3)经CCK8法考察了该类衍生物的体外抗肺纤维化活性.结果显示:该类衍生物都表现出一定抗肺纤维化活性,可作为抗肺纤维化潜在药物进一步研究.
Design,Synthesis and Anti-lung Fibrosis Activities Evaluation of Novel Imidazo[1,2-a]-pyridine Derivatives
Imidazole[1,2-a]-pyridine is an important nucleus for maintaining the activity of various drugs.Structural derivatization of imidazole[1,2-a]-pyridine could be served as an important approach to obtain ATX inhibitors for pulmonary fibrotic diseases treatment.Herein,a novel series of imidazo[1,2-a]-pyridine derivatives(5a~5e,8)were designed and synthesized based on the modification site at the 6-and 3-position of amino group.The structures of all products were characterized by 1H NMR,13C NMR and MS(ESI).Then,the anti-lung fibrosis activities were evaluated in NIH/3T3 cells by CCK8 assay,which indicated that these derivatives exhibited anti-pulmonary fibrosis activity.The results demonstrated that these derivatives could be used as the potential drugs for anti-lung fibrosis.

imidazo[1,2-a]-pyridineATX/LPA axisanti-lung fibrosisactivitysynthesis

何曾亮、邓聪慧、苏兴萍、张啸宇、黄晴菲、王启卫

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中国科学院成都有机化学研究所,四川成都 610041

中国科学院大学,北京 100049

四川大学生物治疗全国重点实验室,四川成都 610041

西华大学理学院,四川成都 610039

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咪唑[1,2-a]-吡啶 ATX/LPA轴 抗肺纤维化 活性 合成

2024

合成化学
四川省化学化工学会 中国科学院成都有机化学研究所

合成化学

CSTPCD
影响因子:0.42
ISSN:1005-1511
年,卷(期):2024.32(12)