新型抗心衰化合物的合成及稳定性研究

Synthesis of A Novel Anti-Heart Failure Compounds and Study on Its Stability

心力衰竭是各类心血管疾病的最终归宿,具有高发病率、高致死率及治疗费用高等特点。通过将异烟酸乙酯与水合肼反应生成异烟肼后与2-羟基-1-萘甲醛两步步反应得到具有细胞活性的小分子化合物——新型心肌肌球蛋白激动剂AFHF001,进而采用质谱法和核磁共振技术对其进行结构确证。对其稳定性考察发现其在酸性条件及碱性生理盐水中不稳定,易发生分解。该合成方法快速简便,分子结构准确可靠,稳定性考察可为后续临床试验提供数据支撑。

Heart failure is the ultimate destination of various types of cardiovascular diseases,with high morbidity,high mortality and high treatment costs. After reacting ethyl is nicotinate with hydrazine hydrate to produce isoniazid,a two-step reaction with 2-hydroxy-1-naphthaldehyde was performed to obtain a cell-active small molecule compound-a novel cardiac myosin agonist AF-HF001. Furthermore,the structure was confirmed by mass spectrometry and nuclear magnetic resonance. Its stability was found to be unstable in acidic conditions and alkaline saline,and it was prone to decomposition. The synthesis method was quick and easy,the molecular structure was accurate and reliable,and the stability inspection can provide data support for follow-up clinical trials.