Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic

DOI: 10.1016/j.bmcl.2009.06.065

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 4711 - 4714 (2009)

Update date:2022-08-04

Topics: Synthesis Design Experimental terms

Authors:

Wangsell, Fredrik

Russo, Francesco

Saevmarker, Jonas

Rosenquist, Asa

Samuelsson, Bertil

Larhed, Mats

Read Full Text PDF DownLoad Join now for total 90,000,000 free articles

Article abstract of DOI:10.1016/j.bmcl.2009.06.065

Two series of drug-like BACE-1 inhibitors with a shielded tertiary hydroxyl as transition state isostere have been synthesized. The most potent inhibitor exhibited a BACE-1 IC₅₀ value of 0.23 μM.

Full text of DOI:10.1016/j.bmcl.2009.06.065

Products guided by the article

Product name:2-hydroxy-2-phenethylpentanedioic acid 5-[((S)-1-benzylcarbamoyl-2-methylpropyl)amide] 1-{[3-[(R)-1-(4-fluorophenyl)ethylcarbamoyl]-5-(methanesulfonyl(methyl)amino)phenyl]amide}

Cas No:1187975-77-4

R&D Labs maybe for 1187975-77-4

Nanjing Capatue Chemical Co., Ltd

Contact:+86-25-86371192 +86-025-85720158

Address:No.20 Jiangjun Avenue, Jiangning Economic & Technical Development Zone
Zibo Xiaoguang Chemical Material Co., Ltd

Contact:15954099116

Address:Boshan Development Zone
Hangzhou Zyter Biological & Chemical Technology Co., Ltd.

website:http://www.zyterpharm.com

Contact:+86-18858184290

Address:West Wenyi Road, Cangqian, Yuhang
Shijiazhuang Haitian Amino Acid Co., Ltd.

Contact:+86-311-88908111

Address:Shijiazhuang Hebei province,China
zhengzhou Triz Pharma-Tech Co., Ltd

website:http://www.Trizpharma-tech.com

Contact:+86-0371-86597269，53392065

Address:High-tech Industrial Development Zone, Zhengzhou City, NO.7 Holly Street

Relevant to this article

Highly Reactive and Stereoselective (R)- and (S)-3-(N,N-Dimethylcarbamoyl)-1,2,4-trimethyl-1,4-dihydropyridines for NADH-NAD⁺ Mimicry

Doi:10.1021/jo00267a016
(1989)
α-Spiro endoperoxides: synthesis and evaluation of their antimalarial activities

Doi:10.1016/j.tet.2009.07.030
(2009)
Enantioselective allylation, crotylation, and reverse prenylation of substituted isatins: Iridium-catalyzed C - C bond-forming transfer hydrogenation

Doi:10.1002/anie.200902328
(2009)
Halogenation of fluorinated cyclic 1,3-dicarbonyl compounds: new aspects of synthetic application

Doi:10.1016/j.tet.2009.06.122
(2009)
Formylation of Allylsilanes: A Synthesis of β,γ-Unsaturated Aldehyde Acetals

Doi:10.1055/s-1989-27171
(1989)
La(OTf)₃: An efficient promoter for thioglycoside activation in conjunction with N-iodosuccinimide

Doi:10.1055/s-0030-1259016
(2010)

Article Doi