细菌脲酶抑制剂及其作用机理的研究进展

Research Progress in Urease Inhibitors and Its Mechanism

脲酶抑制剂能有效抑制细菌脲酶活性,降低尿素分解菌产生氨的速度,广泛应用于医药及农业领域。然而,目前使用的脲酶抑制剂存在着生物毒性强、微生物适应性与稳定性差等问题,限制了脲酶抑制剂的应用。近年来,研究发现了一系列新的脲酶抑制先导化合物,同时报道了这些化合物的脲酶抑制结构以及作用模式与机制。本文综述了近10年有关脲酶抑制剂的报道,并对所报道的脲酶抑制剂进行系统分类,以探讨不同类别的脲酶抑制剂的构效关系、抑制效果与抑制模式,并从不同类型脲酶抑制剂的构效关系探讨了其作用机理,旨在为新型脲酶抑制剂的开发提供参考。

Urease inhibitors suppress urease activity,consequently lower the rate of ureolytic process between the urease producing bacteria and urea.Urease inhibitor has been widely implemented in both agriculture and medical area.But the existing bacterial urease inhibitor holds a lot of downsides such as toxicity,microbial adaptation,and compromised stability.These problems limit the application of urease inhibitors.In recent years,a lot of novel urease inhibitors have been found and its motifs and substructures bearing urease inhibition capacity have been revealed.The related interaction mode and mechanism have also been demonstrated.This article reviews urease inhibitors reported in the past ten years;arranges them in different groups and discusses the structure-activity relationship,inhibition effectiveness,and inhibition mode of individual groups.The inhibition mechanism was discussed from the perspective of structure-activity relationship of different types of urease inhibitors.This article may serve as useful reference for future discovery of novel urease inhibitor.