Aβ Aggregation inhibitors. Part 1: Synthesis and biological activity of phenylazo benzenesulfonamides

Shwu Jiuan Lin; Young Ji Shiao; Chih Wen Chi; Li Ming Yang

doi:10.1016/j.bmcl.2003.12.086

Aβ Aggregation inhibitors. Part 1: Synthesis and biological activity of phenylazo benzenesulfonamides

Shwu Jiuan Lin, Young Ji Shiao, Chih Wen Chi, Li Ming Yang

Research output: Contribution to journal › Article › peer-review

24 Citations (Scopus)

Abstract

Phenylazo benzenesulfonamides were designed and synthesized as β-amyloid (Aβ₄₀) fibril assembly inhibitors, and evaluated for inhibition of Aβ₄₀ aggregation and neurotoxicity using rat cortical neurons. Compound 2 (LB-152) was the most potent compound in this study, and the para-NMe₂ group on the end of the phenylazo moiety may play an important role in preventing Aβ₄₀ fibril formation. LB-152 provides a new lead for further development of potential β-amyloid aggregation inhibitors to treat AD.

Original language	English
Pages (from-to)	1173-1176
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	5
DOIs	https://doi.org/10.1016/j.bmcl.2003.12.086
Publication status	Published - Mar 8 2004

Keywords

Alzheimer's disease
Benzenesulfonamide
beta-Amyloid
Phenylazo

ASJC Scopus subject areas

Biochemistry
Molecular Biology
Organic Chemistry
Drug Discovery
Pharmaceutical Science

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10.1016/j.bmcl.2003.12.086

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title = "Aβ Aggregation inhibitors. Part 1: Synthesis and biological activity of phenylazo benzenesulfonamides",

abstract = "Phenylazo benzenesulfonamides were designed and synthesized as β-amyloid (Aβ40) fibril assembly inhibitors, and evaluated for inhibition of Aβ40 aggregation and neurotoxicity using rat cortical neurons. Compound 2 (LB-152) was the most potent compound in this study, and the para-NMe2 group on the end of the phenylazo moiety may play an important role in preventing Aβ40 fibril formation. LB-152 provides a new lead for further development of potential β-amyloid aggregation inhibitors to treat AD.",

keywords = "Alzheimer's disease, Benzenesulfonamide, beta-Amyloid, Phenylazo, Alzheimer's disease, Benzenesulfonamide, beta-Amyloid, Phenylazo",

author = "Lin, {Shwu Jiuan} and Shiao, {Young Ji} and Chi, {Chih Wen} and Yang, {Li Ming}",

year = "2004",

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doi = "10.1016/j.bmcl.2003.12.086",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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T1 - Aβ Aggregation inhibitors. Part 1

T2 - Synthesis and biological activity of phenylazo benzenesulfonamides

AU - Lin, Shwu Jiuan

AU - Shiao, Young Ji

AU - Chi, Chih Wen

AU - Yang, Li Ming

PY - 2004/3/8

Y1 - 2004/3/8

N2 - Phenylazo benzenesulfonamides were designed and synthesized as β-amyloid (Aβ40) fibril assembly inhibitors, and evaluated for inhibition of Aβ40 aggregation and neurotoxicity using rat cortical neurons. Compound 2 (LB-152) was the most potent compound in this study, and the para-NMe2 group on the end of the phenylazo moiety may play an important role in preventing Aβ40 fibril formation. LB-152 provides a new lead for further development of potential β-amyloid aggregation inhibitors to treat AD.

AB - Phenylazo benzenesulfonamides were designed and synthesized as β-amyloid (Aβ40) fibril assembly inhibitors, and evaluated for inhibition of Aβ40 aggregation and neurotoxicity using rat cortical neurons. Compound 2 (LB-152) was the most potent compound in this study, and the para-NMe2 group on the end of the phenylazo moiety may play an important role in preventing Aβ40 fibril formation. LB-152 provides a new lead for further development of potential β-amyloid aggregation inhibitors to treat AD.

KW - Alzheimer's disease

KW - Benzenesulfonamide

KW - beta-Amyloid

KW - Phenylazo

KW - Alzheimer's disease

KW - Benzenesulfonamide

KW - beta-Amyloid

KW - Phenylazo

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 5

ER -

Aβ Aggregation inhibitors. Part 1: Synthesis and biological activity of phenylazo benzenesulfonamides

Abstract

Keywords

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