(1,3)-β-D-葡聚糖合成酶小分子抑制剂研究进展

Recent progress of small-molecule(1,3)-β-Dglucan synthase inhibitors

(1,3)-β-D-葡聚糖合成酶抑制剂通过破坏真菌细胞壁的合成而产生特异性的抗真菌作用。目前上市的(1,3)-β-D-葡聚糖合成酶抑制剂均为环六脂肽类,只能通过静脉注射给药。研发合成简便、可口服的(1,3)-β-D-葡聚糖合成酶小分子抑制剂具有巨大的研究前景。本文综述了近年来葡聚糖合成酶小分子抑制剂的研究进展。

（ 1,3 ）-β-D-glucan synthase（ GS ） inhibitors exert their fungicidal activity through a totally differ- ent mechanism from the amB and the azoles by disrupting the cell wall skeleton. GS inhibitors approved for clinical use are macrocyclic hexapeptides, which are used only for parenteral administration. Thus, the dis- covery and optimization of synthetically convenient and orally bioavailable small-molecule GS inhibitors have a promising future. In this review, recent progress of small-molecule GS inhibitors was summarized.