Chioua Mourad, Samadi Abdelouahid, Soriano Elena, Lozach Olivier, Meijer Laurent, Marco-Contelles José
Laboratorio de Radicales Libres y Química Computacional (IQOG, CSIC), 28006 Madrid, Spain.
Bioorg Med Chem Lett. 2009 Aug 15;19(16):4566-9. doi: 10.1016/j.bmcl.2009.06.099. Epub 2009 Jul 3.
The synthesis and biological evaluation of a number of differently substituted 3,6-diamino-1H-pyrazolo[3,4-b]pyridine derivatives are reported. From the inhibition results on a selection of disease-relevant protein kinases [IC(50) (microM) DYRK1A=11; CDK5=0.41; GSK-3=1.5] we have observed that 3,6-diamino-4-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile (4) constitutes a potential new and simple lead compound in the search of drugs for the treatment of Alzheimer's disease.
报道了多种不同取代的3,6-二氨基-1H-吡唑并[3,4-b]吡啶衍生物的合成及生物学评价。根据对一系列与疾病相关的蛋白激酶的抑制结果[IC(50)(μM):DYRK1A = 11;CDK5 = 0.41;GSK-3 = 1.5],我们观察到3,6-二氨基-4-苯基-1H-吡唑并[3,4-b]吡啶-5-腈(4)在寻找治疗阿尔茨海默病的药物方面构成了一种潜在的新型简单先导化合物。