Tricyclic sulfones as orally active gamma-secretase inhibitors: synthesis and structure-activity relationship studies.

ID: ALA1158621

Journal: Bioorg Med Chem Lett

Title: Tricyclic sulfones as orally active gamma-secretase inhibitors: synthesis and structure-activity relationship studies.

Authors: Sasikumar TK, Qiang L, Burnett DA, Cole D, Xu R, Li H, Greenlee WJ, Clader J, Zhang L, Hyde L.

Abstract: Tricyclic sulfones were designed as gamma-secretase inhibitors and found to have excellent potency. Extensive SAR shows that a large number of sulfonamides at position 7 of the tricycle are very well tolerated. Compounds such as 15a and 15c showed remarkable in vivo potency.

CiteXplore: 20493690

DOI: 10.1016/j.bmcl.2010.04.104

Patent ID: ┄