Newly-created fluorenone drugs can be used to prevent, treat, or otherwise reduce damage to a brain or spinal cord following a medical crisis. These new drugs are markedly improved analogs of previously-known fluorenone compounds that were never commercialized or developed into medically useful treatments. The new analogs have the following structure:
where X is a lower alkyl, substituted alkyl, or cycloalkyl group, R is selected from certain types of ether, ester, or amide groups, and Y1 and Y2 are halogen, hydrogen, or methyl. These new compounds can penetrate a blood-brain barrier and potently inhibit the unwanted release of excitotoxic neurotransmitters by astrocyte cells following an injury or insult to the brain or spinal cord. As an illustration, some of these new analogs were more than 30 times more potent than the previously known best compound in reducing aspartate release by stressed astrocytes. The new analogs also reduce swelling in astrocytes, thereby promoting proper blood flow through the brain and spinal cord following an injury or other crisis. These new analogs have been shown to work with very good efficacy in in vivo animal models of focal or global brain ischemia.
新创建的荧
酮类药物可以用于预防、治疗或减少医疗危机后对大脑或脊髓的损伤。这些新药物是以前未商业化或开发成医疗有用治疗方法的荧
酮类化合物的明显改进类似物。新的类似物具有以下结构:其中X是低烷基,取代烷基或环烷基,R是从某些类型的醚,酯或酰胺基团中选择的,Y1和Y2是卤素,氢或甲基。这些新化合物可以穿过血脑屏障,并有效地抑制星形胶质细胞在大脑或脊髓受损或受伤后不想要的兴奋性神经递质的释放。例如,这些新类似物中的一些在减少应力星形胶质细胞释放
天冬氨酸方面比先前已知的最佳化合物强30倍以上。新的类似物还可以减少星形胶质细胞的肿胀,从而促进受损或危机后大脑和脊髓的适当血流。这些新类似物已经在局部或全局脑缺血的体内动物模型中表现出非常好的功效。