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

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.

journal_name

Bioorg Med Chem Lett

authors

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

doi

10.1016/j.bmcl.2010.04.104

subject

Has Abstract

pub_date

2010-06-15 00:00:00

pages

3632-5

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00574-3

journal_volume

20

pub_type

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