Carbocyclic [g] indole inhibitors of human nonpancreatic s-PLA2

…, DW Snyder, MK Chastain, RL Tielking…

文献索引：Sawyer, J. Scott; Beight, Douglas W.; Smith, Edward C. R.; Snyder, David W.; Chastain, Marcia K.; Tielking, Richard L.; Hartley, Lawrence W.; Carlson, Donald G. Journal of Medicinal Chemistry, 2005 , vol. 48, # 3 p. 893 - 896

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被引用次数: 18

摘要

A vinyl azide cyclization method was used to synthesize three different carbocyclic [g] indole scaffolds as inhibitors of human nonpancreatic secretory phospholipase A2. Each scaffold demonstrated potent enzyme activity in a chromogenic assay system, with select examples also demonstrating potent activity in a secondary DOC/PC assay. Compound 11, representative of the cyclopent [g] indole series, gave an IC50 of 10 nM for the inhibition of ...