Ketol-acid reductoisomerase: An important antituberculosis drug target

由于耐药性的日益普遍，迫切需要新的抗结核药物。在这里，我们将使用合理的结构为基础的方法来设计新的抑制剂酮醇酸还原异构酶（KARI），一种酶的活性是必不可少的生存这种病原体，驻留在人类的肺部。这些抑制剂将被转化为前药制剂，以在基于细胞的测定和感染该病原体的小鼠中获得最佳活性。

Due to the increasing prevalence of drug resistance, new antituberculosis medications are urgently needed. Here, we will use rational structure-based approaches to design new inhibitors of ketolacid reductoisomerase (KARI), an enzyme whose activity is essential to the survival of this pathogen that resides in the lungs of humans. These inhibitors will be converted into prodrug formulations for optimal activity in cell-based assays and in mice infected with this pathogen.