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KMID : 0606320080240010022
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Journal of Phamacetical Sciences Sookmyung Women s University
2008 Volume.24 No. 1 p.22 ~ p.26
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Design and Synthesis of 2-(4-tert-butylphenoxy)-N-(3-fluoro-4-methanesulfonylaminobenzyl)-N’-hydroxyacetamidine as a TRPV1 antagonist
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Kong Hye-Kyung
Kim Hee-Doo
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Abstract
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2-(4-tert-butylphenoxy)-N-(3-fluoro-4-methanesulfonylaminobenzyl)-N’-hydroxyacetamidine(10) was designed, synthesized and evaluated as a TRPV1 antagonist. Amidine group was introduced as a bioisoster of amide to improve the pharmacological profile. Compound 9 showed an antagonist activity with 2.8 μM of IC_(50) value in ^(45)Ca²^(+)-influx assay.
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KEYWORD
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TRPV1, antagonist, amidine, bioisoster, ^(45)Ca²^(+)-influx assay
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