Carbocyclic[g]indole inhibitors of human nonpancreatic s-PLA2.
作者信息
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
机构信息
Discovery Chemistry Research and Technology, The Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA.
出版信息
J Med Chem. 2005 Feb 10;48(3):893-6. doi: 10.1021/jm0401309.
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 hnps-PLA2 in the chromogenic assay.
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