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作为γ-分泌酶抑制剂的N-(5-氯-2-(羟甲基)-N-烷基-芳基磺酰胺)

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

作者信息

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

机构信息

Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA.

出版信息

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4432-6. doi: 10.1016/j.bmcl.2007.06.022. Epub 2007 Jun 10.

DOI:10.1016/j.bmcl.2007.06.022
PMID: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.

摘要

一系列N-烷基苯磺酰胺是从高通量筛选得到的活性化合物发展而来的。采用经典和并行合成策略来制备具有良好体外和体内γ-分泌酶活性的化合物。

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