Novel pyrrole-and 1, 2, 3-triazole-based 2, 3-oxidosqualene cyclase inhibitors

T Watanabe, Y Umezawa, Y Takahashi…

文献索引：Watanabe, Takumi; Umezawa, Yoji; Takahashi, Yoshikazu; Akamatsu, Yuzuru Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 19 p. 5807 - 5810

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被引用次数: 15

摘要

Pyrrole-and 1, 2, 3-triazole-based 2, 3-oxidosqualene cyclase (OSC) inhibitors 3 and 4 were discovered by conducting a virtual screening, a docking study based on the crystallographic structure of OSC, and biological assays. The hit rate of the assays was increased by establishing appropriate substructural filters in the virtual screening stage. Amide derivatives of 8 and 12 preserved the inhibitory activity of parent compound 3, which provided a ...