Lead Evolution in Development of an Anti-allergic Agent ; Dimethyl(2-phenoxyethyl)sulfonium p-Toluenesulfonate as the Secondary Lead Compound

Derivatives of 2-hydroxyethyldimethylsulfonium p-toluenesulfonate (1) were evaluated for anti-allergic activity in order to develop the drug for treatment of type I allergic diseases. The IgE-induced rat homologous passive cutaneous anaphylaxis (PCA) was inhibited by some 2-alkoxy and 2-aryloxyethyl...

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Published inChem-Bio Informatics Journal Vol. 2; no. 3; pp. 86 - 94
Main Authors Tada, Yukio, Yamawaki, Ichiro, Ueda, Shuichi, Matsumoto, Hiroshi, Matsuura, Naosuke, Yasumoto, Mitsugi, Koda, Akihide, Hori, Mikio
Format Journal Article
LanguageEnglish
Published Tokyo Chem-Bio Informatics Society 2002
Japan Science and Technology Agency
Subjects
antialllergic activity
lead evolution
QSAR
sulfonium p-toluenesulfonate
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Summary:Derivatives of 2-hydroxyethyldimethylsulfonium p-toluenesulfonate (1) were evaluated for anti-allergic activity in order to develop the drug for treatment of type I allergic diseases. The IgE-induced rat homologous passive cutaneous anaphylaxis (PCA) was inhibited by some 2-alkoxy and 2-aryloxyethyl sulfonium p-toluenesulfonates. There were some correlations between hydrophobicity or electronic properties (HOMO or charge at the O atom) and anti-allergic activity or acute toxicity. Dimethyl(2-phenoxyethyl)sulfonium p-toluenesulfonate (5) was selected as a second lead compound in the next stage.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-1
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ISSN:1347-6297
1347-0442
DOI:10.1273/cbij.2.86