CHEMICALLY CONJUGATED TRANSPORTORS FOR LOW HYDROPHOBIC BIOACTIVE DRUGS

The present disclosure provides a compound comprising a modified tetracycline derivative covalently coupled to a low hydrophobic biologically active molecule for use in the treatment of neurodegenerative diseases through a linker defined by the general formula XZX, in particular, a compound comprising a modified tetracycline derivative covalently coupled to a low hydrophobic biologically active molecule for use in the treatment of neurodegenerative diseases, wherein the modified tetracycline derivative is a chemically modified doxycycline derivative and the low hydrophobic bioactive molecule for use in the treatment of neurodegenerative diseases is dopamine. The disclosure also provides methods of making such compounds, as well as methods of treating neurodegenerative diseases comprising administering the compounds. 本公开提供一种化合物，其包含经修饰的四环素衍生物，所述经修饰的四环素衍生物通过由通式XZX定义的接头与用于治疗神经退行性疾病的低疏水性生物活性分子共价偶联，特别地提供这样的化合物，其中所述经修饰的四环素衍生物是经化学修饰的多西环素衍生物且所述用于治疗神经退行性疾病的低疏水性生物活性分子是多巴胺。本公开还提供制备这种化合物的方法，以及治疗神经退行性疾病的方法，其包括施用所述化合物。