Design and optimization of tricyclic gamma-secretase modulators. Issue 5 (1st March 2016)

• Record Type: Journal Article
• Authors: Shi, Jianliang; Zuev, Dmitry; Xu, Li; Lentz, Kimberley A.; Grace, James E.; Toyn, Jeremy H.; Olson, Richard E.; Macor, John E.; Thompson, Lorin A.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 5(2016)
• Page Start: 1498
• Page End: 1502
• Publication Date: 2016-03-01
• Subjects: Alzheimer's disease -- Gamma-secretase modulators -- CYP3A4 inhibition; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.06.020
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Beginning with a diaminotriazine screening hit, several series of novel, tricyclic gamma-secretase modulators (GSMs) were designed. The SAR of several related series of GSMs is presented, and the in vivo profile of a lead molecule from the series is described.