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在三氯氧磷催化下,6种3-脂肪基-1,2,4-三唑(1a~1f)和3-苯基-1,2,4-三唑(1g)分别与对苯二甲酸和2-氨基-1,4-对苯二甲酸发生环化反应,高产率合成了14种双枝三唑并噻二唑稠环衍生物(2和3),并对其进行了结构表征及药物活性测试.目标化合物对Cdc25B和PTP1B抑制活性筛选结果表明,化合物2f,3a和3g对Cdc25B有较高的抑制活性,IC50值分别为(3.45±0.60),(0.69±0.10)和(1.52±0.19)μg/mL;化合物3a和3b对PTP1B表现出较高的抑制活性,IC50值分别为(0.98±0.13)和(2.00±0.16)μg/mL.
Under the phosphorus oxychloride catalysis, 6 kinds of 3-aliphatic-1,2,4-triazole (1a ~ 1f) and 3-phenyl-1,2,4-triazole (1g) Formic acid and 2-amino-1,4-terephthalic acid cyclization reaction, synthesis of 14 kinds of bi-branched triazolothiadiazole fused ring derivatives (2 and 3), and its structural characterization The results showed that compounds 2f, 3a and 3g had a higher inhibitory activity on Cdc25B with IC50 values of (3.45 ± 0.60), (0.69 ± 0.10) and (1.52 ± 0.19) μg / mL. Compounds 3a and 3b showed high inhibitory activity against PTP1B with IC50 values of (0.98 ± 0.13) and (2.00 ± 0.16) μg / mL, respectively.