title: Nitrogen-appended N-alkylsulfonamides as inhibitors of gamma-secretase.
abstract: The synthesis and gamma-secretase inhibition data for a series of nitrogen-appended N-alkylsulfonamides (11-47) are described. Inhibition of brain Abeta in transgenic mice was demonstrated by two of these compounds (23 and 44).
authors.affiliation: Department of Discovery Chemistry, Research and Development, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA. carl.bergstrom@bms.com
authors.forename: Carl P
authors.initials: CP
authors.lastname: Bergstrom
authors.forename: Charles P
authors.initials: CP
authors.lastname: Sloan
authors.forename: Henry H
authors.initials: HH
authors.lastname: Wang
authors.forename: Michael F
authors.initials: MF
authors.lastname: Parker
authors.forename: David W
authors.initials: DW
authors.lastname: Smith
authors.forename: Ming
authors.initials: M
authors.lastname: Zheng
authors.forename: Steven B
authors.initials: SB
authors.lastname: Hansel
authors.forename: Craig T
authors.initials: CT
authors.lastname: Polson
authors.forename: Lauren E
authors.initials: LE
authors.lastname: Barber
authors.forename: Isia
authors.initials: I
authors.lastname: Bursuker
authors.forename: Valerie L
authors.initials: VL
authors.lastname: Guss
authors.forename: Jason A
authors.initials: JA
authors.lastname: Corsa
authors.forename: Donna M
authors.initials: DM
authors.lastname: Barten
authors.forename: Kevin M
authors.initials: KM
authors.lastname: Felsenstein
authors.forename: Susan B
authors.initials: SB
authors.lastname: Roberts
mesh_terms: D000478:Alkylation; D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors*; D016229:Amyloid beta-Peptides / Q000235:genetics / Q000378:metabolism; D000818:Animals; D001393:Azoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001921:Brain / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism; D057927:Hydrophobic and Hydrophilic Interactions; D020128:Inhibitory Concentration 50; D051379:Mice; D008822:Mice, Transgenic; D010446:Peptide Fragments / Q000378:metabolism; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000588:Amines; D016229:Amyloid beta-Peptides; D001393:Azoles; D010446:Peptide Fragments; D011480:Protease Inhibitors; D013449:Sulfonamides; C078592:amyloid beta-protein (1-40); D053829:Amyloid Precursor Protein Secretases