Bristol-Myers Squibb Pharmaceutical Research Institute, Bristol-Myers Squibb, PO Box 4000, Princeton, NJ 08543, USA. david.weinstein@bms.com
Abstract:
A series of inhibitors of mammalian 15-lipoxygenase based on tryptamine and homotryptamine scaffolds is described. Compounds with aryl substituents at C-2 of the indole core of tryptamine and homotryptamine sulfonamides (e.g., 37a-p) proved to be potent inhibitors of the isolated enzyme. Selected compounds also demonstrated desirable inhibition selectivities over isozymes 5- and P-12-LO.