disorders. In this study, we introduced the pharmacophore of fibrates to a BRD4 inhibitor, RVX-208, to design dual-active hypolipidemic compounds, and found that some of new analogues showed favorable hypolipidemic activities. Synthetic accessibility towards this class of compounds optimized RVX-208 as well as would supply more thoughts on hypolipidemic drugs.
含
溴结构域蛋白4(BR
D4)是一种新的治疗靶标,用于治疗包括心血管疾病,癌症,炎症和中枢神经系统(CNS)疾病在内的各种疾病。在这项研究中,我们将贝特类药物的药效团引入了BR
D4抑制剂RVX-208,以设计具有双重活性的降血脂化合物,并发现一些新的类似物具有良好的降血脂活性。这类化合物的合成可及性优化了
RVX-208,并为降血脂药提供了更多的思路。