Carbocyclic[g]indole Inhibitors of Human Nonpancreatic s-PLA2
Journal of Medicinal Chemistry2005Vol. 48(3), pp. 893–896
Citations Over Time
J. Scott Sawyer, Douglas W. Beight, Edward C. Smith, David W. Snyder, Marcia K. Chastain, Richard L. Tielking, Lawrence W. Hartley, Donald G. Carlson
Abstract
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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