DprE1抑制剂抗结核新药研究进展

Research progress of DprE1 inhibitors as new anti-tuberculosis drugs

结核病尤其是耐药结核病仍然是威胁人类健康的主要传染病之一。目前临床上使用的不少抗结核药物存在治疗效果差、成本高和副作用大等缺点。因此迫切需要开发新的、更安全的、更有效和毒性更低,且具有崭新作用机制的抗结核药物。近年来,DprE1抑制剂类药物在抗结核作用中的研究取得了一定的进展。DprE1抑制剂类药物的作用靶点位于结核分枝杆菌的细胞壁,通过抑制结核分枝杆菌细胞壁DprE1,从而抑制结核分枝杆菌的生长。笔者就DprE1抑制剂的类别、作用机制、抗菌活性、药代动力学和药效动力学、动物实验、临床试验、安全性、有效性等方面的研究进展做一综述。

Tuberculosis continues to be one of the most serious infectious diseases threatening human health.At the moment,clinical use of anti-tuberculosis drugs has a poor therapeutic effect,has a high cost,has side effects,and has other flaws.As a result,there is an urgent need to develop new antitubercular drugs with new mechanism of action that are safer,more widely effective,and less toxic.Some progress has been made in the study of DprE1 inhibitors′anti-tuberculosis effect in recent years.DprE1 inhibitors target the cell wall of mycobacterium tuberculosis and inhibit its growth by inhibiting the DprE1 enzyme that produces the mycobacterium tuberculosis cell wall.This paper reviewed DprE1 inhibitors interms of classification,mechanism of action,antimicrobial activity,pharmacokinetics and pharmacodynamics,as well as drug safety,animal experiments,and clinical trials.