N-(5-chloro-2-(hydroxymethyl)-N-alkyl-arylsulfonamides as gamma-secretase inhibitors.

Parker, Michael F; Barten, Donna M; Bergstrom, Carl P; Bronson, Joanne J; Corsa, Jason A; Deshpande, Milind S; Felsenstein, Kevin M; Guss, Valerie L; Hansel, Steven B; Johnson, Graham; Keavy, Daniel J; Lau, Wai Y; Mock, Jeremy; Prasad, C V C; Polson, Craig T; Sloan, Charles P; Smith, David W; Wallace, Owen B; Wang, Henry H; Williams, Andrew; Zheng, Ming

Parker, Michael F; Barten, Donna M; Bergstrom, Carl P; Bronson, Joanne J; Corsa, Jason A; Deshpande, Milind S; Felsenstein, Kevin M; Guss, Valerie L; Hansel, Steven B; Johnson, Graham; Keavy, Daniel J; Lau, Wai Y; Mock, Jeremy; Prasad, C V C; Polson, Craig T; Sloan, Charles P; Smith, David W; Wallace, Owen B; Wang, Henry H; Williams, Andrew; Zheng, Ming.

Affiliation

Parker MF; Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA. parkerm@BMS.com

Bioorg Med Chem Lett ; 17(16): 4432-6, 2007 Aug 15.

Article in En | MEDLINE | ID: mdl-17606371

ABSTRACT

A series of N-alkylbenzenesulfonamides were developed from a high throughput screening hit. Classic and parallel synthesis strategies were employed to produce compounds with good in vitro and in vivo gamma-secretase activity.

Subject(s)

Amyloid Precursor Protein Secretases/antagonists & inhibitors; Sulfonamides/chemistry; Sulfonamides/pharmacology; Amyloid beta-Peptides/metabolism; Animals; Brain/drug effects; Brain/metabolism; Mice; Mice, Transgenic; Molecular Structure; Protein Binding

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Collection: 01-internacional Database: MEDLINE Main subject: Sulfonamides / Amyloid Precursor Protein Secretases Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2007 Type: Article Affiliation country: United States

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