Synthesis of 1,3-diphenyl-2-propen-1-one derivatives and evaluation of their biological activities

Soyong Jang; Jae Chul Jung; Seikwan Oh

doi:10.1016/j.bmc.2007.03.077

Synthesis of 1,3-diphenyl-2-propen-1-one derivatives and evaluation of their biological activities

Soyong Jang, Jae Chul Jung, Seikwan Oh

Department of Molecular Medicine

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

18 Scopus citations

Abstract

A simple synthesis and biological properties of 1,3-diphenyl-2-propen-1-ones 18-22 and 25-26 are described. The key synthetic strategies involve Grignard reaction of aldehyde 2 and oxidation reaction of 8-12 in high yields. The prepared compounds 18-22 and 25-26 were evaluated for free-radical scavenging, suppression of LPS-induced NO generation, and anti-excitotoxicity in vitro. It was found that a couple of compounds, especially 21 and 26, were potent suppressors of NO generation and demonstrated anti-excitotoxicity with the concentration range 10-20 μM in vitro.

Original language	English
Pages (from-to)	4098-4105
Number of pages	8
Journal	Bioorganic and Medicinal Chemistry
Volume	15
Issue number	12
DOIs	https://doi.org/10.1016/j.bmc.2007.03.077
State	Published - 15 Jun 2007

Bibliographical note

Funding Information:
This work has been supported by KOSEF Brain Neurobiology Grant (2006).

Keywords

1,3-Diphenyl-2-propen-1-ones
Anti-excitotoxicity
Grignard reaction
NO-generation

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10.1016/j.bmc.2007.03.077

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title = "Synthesis of 1,3-diphenyl-2-propen-1-one derivatives and evaluation of their biological activities",

abstract = "A simple synthesis and biological properties of 1,3-diphenyl-2-propen-1-ones 18-22 and 25-26 are described. The key synthetic strategies involve Grignard reaction of aldehyde 2 and oxidation reaction of 8-12 in high yields. The prepared compounds 18-22 and 25-26 were evaluated for free-radical scavenging, suppression of LPS-induced NO generation, and anti-excitotoxicity in vitro. It was found that a couple of compounds, especially 21 and 26, were potent suppressors of NO generation and demonstrated anti-excitotoxicity with the concentration range 10-20 μM in vitro.",

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author = "Soyong Jang and Jung, {Jae Chul} and Seikwan Oh",

note = "Funding Information: This work has been supported by KOSEF Brain Neurobiology Grant (2006).",

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doi = "10.1016/j.bmc.2007.03.077",

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T1 - Synthesis of 1,3-diphenyl-2-propen-1-one derivatives and evaluation of their biological activities

AU - Jang, Soyong

AU - Jung, Jae Chul

AU - Oh, Seikwan

N1 - Funding Information: This work has been supported by KOSEF Brain Neurobiology Grant (2006).

PY - 2007/6/15

Y1 - 2007/6/15

N2 - A simple synthesis and biological properties of 1,3-diphenyl-2-propen-1-ones 18-22 and 25-26 are described. The key synthetic strategies involve Grignard reaction of aldehyde 2 and oxidation reaction of 8-12 in high yields. The prepared compounds 18-22 and 25-26 were evaluated for free-radical scavenging, suppression of LPS-induced NO generation, and anti-excitotoxicity in vitro. It was found that a couple of compounds, especially 21 and 26, were potent suppressors of NO generation and demonstrated anti-excitotoxicity with the concentration range 10-20 μM in vitro.

AB - A simple synthesis and biological properties of 1,3-diphenyl-2-propen-1-ones 18-22 and 25-26 are described. The key synthetic strategies involve Grignard reaction of aldehyde 2 and oxidation reaction of 8-12 in high yields. The prepared compounds 18-22 and 25-26 were evaluated for free-radical scavenging, suppression of LPS-induced NO generation, and anti-excitotoxicity in vitro. It was found that a couple of compounds, especially 21 and 26, were potent suppressors of NO generation and demonstrated anti-excitotoxicity with the concentration range 10-20 μM in vitro.

KW - 1,3-Diphenyl-2-propen-1-ones

KW - Anti-excitotoxicity

KW - Grignard reaction

KW - NO-generation

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AN - SCOPUS:34247587038

SN - 0968-0896

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JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 12

ER -

Synthesis of 1,3-diphenyl-2-propen-1-one derivatives and evaluation of their biological activities

Abstract

Bibliographical note

Keywords

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