Tricyclic sulfones as orally active γ-secretase inhibitors: Synthesis and structure-activity relationship studies

Article abstract of DOI:10.1016/j.bmcl.2010.04.104

Tricyclic sulfones were designed as γ-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.