Search | VHL Regional Portal

Carbamate-appended N-alkylsulfonamides as inhibitors of gamma-secretase.

Bergstrom, Carl P; Sloan, Charles P; Lau, Wai-Yu; Smith, David W; Zheng, Ming; Hansel, Steven B; Polson, Craig T; Corsa, Jason A; Barten, Donna M; Felsenstein, Kevin M; Roberts, Susan B.

Bioorg Med Chem Lett ; 18(2): 464-8, 2008 Jan 15.

Article in English | MEDLINE | ID: mdl-18178084

ABSTRACT

The synthesis and gamma-secretase inhibition data for a series of carbamate-appended N-alkylsulfonamides are described. Carbamate 54 was found to significantly reduce brain Abeta in transgenic mice. 54 was also found to possess markedly improved brain levels in transgenic mice compared to previously disclosed 1 and 2.

Subject(s)

Amyloid Precursor Protein Secretases/antagonists & inhibitors , Carbamates/chemistry , Protease Inhibitors/chemistry , Protease Inhibitors/pharmacology , Sulfonamides/chemistry , Sulfonamides/pharmacology , Alzheimer Disease/metabolism , Amyloid beta-Peptides/antagonists & inhibitors , Amyloid beta-Peptides/metabolism , Animals , Brain/drug effects , Brain/metabolism , Mice , Mice, Transgenic , Structure-Activity Relationship

ABSTRACT

Subject(s)

SEND TO:

SELECTION OF CITATIONS

SEARCH DETAIL