1450992-57-0Relevant articles and documents
Scaffold hopping of sampangine: Discovery of potent antifungal lead compound against Aspergillus fumigatus and Cryptococcus neoformans
Jiang, Zhigan,Liu, Na,Dong, Guoqiang,Jiang, Yan,Liu, Yang,He, Xiaomeng,Huang, Yahui,He, Shipeng,Chen, Wei,Li, Zhengang,Yao, Jianzhong,Miao, Zhenyuan,Zhang, Wannian,Sheng, Chunquan
, p. 4090 - 4094 (2014)
Discovery of novel antifungal agents against Aspergillus fumigatus and Cryptococcus neoformans remains a significant challenge in current antifungal therapy. Herein the antifungal natural product sampangine was used as the lead compound for novel antifungal drug discovery. A series of D-ring scaffold hopping derivatives were designed and synthesized to improve antifungal activity and water solubility. Among them, the thiophene derivative S2 showed broad-spectrum antifungal activity, particularly for Aspergillus fumigatus and Cryptococcus neoformans. Moreover, compound S2 also revealed better water solubility than sampangine, which represents a promising antifungal lead compound for further structural optimization.