(2 E ,4 E )‐ N ‐(4‐(1 H ‐Indol‐3‐yl)piperidin‐1‐yl)alkyl‐5‐(substituted phenyl)‐2,4‐pentadienamides as Antiallergic Agents with Antihistaminic and Anti Slow‐Reacting Substance (SRS) Activities | Zendy

Shigenaga Shinji | Zendy; Manabe Takashi | Zendy; Matsuda Hiroshi | Zendy; Fujii Takashi | Zendy; Matsuo Masaaki | Zendy

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(2 E ,4 E )‐ N ‐(4‐(1 H ‐Indol‐3‐yl)piperidin‐1‐yl)alkyl‐5‐(substituted phenyl)‐2,4‐pentadienamides as Antiallergic Agents with Antihistaminic and Anti Slow‐Reacting Substance (SRS) Activities

Author(s) -

Shigenaga Shinji,

Manabe Takashi,

Matsuda Hiroshi,

Fujii Takashi,

Matsuo Masaaki

Publication year - 1996

Publication title -

archiv der pharmazie

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.468

H-Index - 61

eISSN - 1521-4184

pISSN - 0365-6233

DOI - 10.1002/ardp.19963290103

Subject(s) - chemistry , in vivo , conjugate , in vitro , histamine , stereochemistry , glucuronic acid , pharmacology , biochemistry , polysaccharide , medicine , mathematical analysis , microbiology and biotechnology , mathematics , biology

As an extension of our study aiming to discover a novel compound with dual activities against histamine and slow‐reacting substance (SRS), we synthesized two types of indolylpiperidine derivatives, 3 and 4–20. Testing for in vivo antianaphylactic activity and for in vitro anti‐SRS activity revealed that (2 E ,4 E )‐5‐(3,5‐dimethoxy‐4‐hydroxyphenyl)‐ N ‐(2‐(4‐(1 H ‐indol‐3‐yl)piperidin‐1‐yl)ethyl)‐2,4‐pentadienamide ( 11 ) exhibited potent dual activities with ED 50 = 0.89 mg/kg and IC 50 = 1.43 μM, respectively. However, the plasma concentration of unchanged 11 was very low when administered orally in guinea pigs. This result can be explained by fast formation of a glucuronic acid conjugate.

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