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

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. (C) 2010 Elsevier Ltd. All rights reserved.