2-(N-Benzyl-N-phenylsulfonamido)alkyl amide derivatives as γ-secretase inhibitors

Michael F Parker; Donna M Barten; Carl P Bergstrom; Joanne J Bronson; Jason A Corsa; Michael F Dee; Yonghua Gai; Valerie L Guss; Mendi A Higgins; Daniel J Keavy; Alice Loo; Robert A Mate; Larry R Marcin; Katharine E McElhone; Craig T Polson; Susan B Roberts; John E Macor

doi:10.1016/j.bmcl.2012.09.057

2-(N-Benzyl-N-phenylsulfonamido)alkyl amide derivatives as γ-secretase inhibitors

Bioorg Med Chem Lett. 2012 Nov 15;22(22):6828-31. doi: 10.1016/j.bmcl.2012.09.057. Epub 2012 Sep 24.

Authors

Michael F Parker¹, Donna M Barten, Carl P Bergstrom, Joanne J Bronson, Jason A Corsa, Michael F Dee, Yonghua Gai, Valerie L Guss, Mendi A Higgins, Daniel J Keavy, Alice Loo, Robert A Mate, Larry R Marcin, Katharine E McElhone, Craig T Polson, Susan B Roberts, John E Macor

Affiliation

¹ Molecular Sciences and Candidate Optimization and Neuroscience Discovery Biology, Bristol-Myers Squibb R&D, 5 Research Parkway, Wallingford, CT 06492, United States. parkerm@bms.com

PMID: 23046960
DOI: 10.1016/j.bmcl.2012.09.057

Abstract

A series of (N-benzyl-N-phenylsulfonamido)alkyl amides were developed from classic and parallel synthesis strategies. Compounds with good in vitro and in vivo γ-secretase activity were identified and described.

MeSH terms

Amides / chemical synthesis
Amides / chemistry*
Amides / metabolism
Amyloid Precursor Protein Secretases / antagonists & inhibitors*
Amyloid Precursor Protein Secretases / metabolism
Amyloid beta-Peptides / metabolism
Peptide Fragments / metabolism
Protease Inhibitors / chemical synthesis
Protease Inhibitors / chemistry*
Protease Inhibitors / metabolism
Protein Binding
Structure-Activity Relationship
Sulfonamides / chemistry*

Substances

Amides
Amyloid beta-Peptides
Peptide Fragments
Protease Inhibitors
Sulfonamides
amyloid beta-protein (1-42)
Amyloid Precursor Protein Secretases