- Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase.
Tryptamine and homotryptamine-based sulfonamides as potent and selective inhibitors of 15-lipoxygenase.
Bioorganic & medicinal chemistry letters (2005-02-17)
David S Weinstein, Wen Liu, Zhengxiang Gu, Charles Langevine, Khehyong Ngu, Leena Fadnis, Donald W Combs, Doree Sitkoff, Saleem Ahmad, Shaobin Zhuang, Xing Chen, Feng-Lai Wang, Deborah A Loughney, Karnail S Atwal, Robert Zahler, John E Macor, Cort S Madsen, Natesan Murugesan
PMID15713402
초록
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.
MATERIALS