87233-54-3Relevant articles and documents
Emedastine hydrochloride intermediate compound and preparation method thereof
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, (2017/09/01)
The invention provides an antihistamine medicine emedastine hydrochloride intermediate and a preparation method thereof, and is used for solving the problems of many reaction steps, operation complexity and high production cost in the preparation process
Synthesis and antihistaminic H1 activity of 1,2,5(6)-trisubstituted benzimidazoles
Goeker, Hakan,Ayhan-Kilcigil, Guelguen,Tuncbilek, Meral,Kus, Canan,Ertan, Rahmiye,Kendi, Engin,Oezbey, Sueheyla,Fort, Merce,Garcia, Celia,Farre, Antonio J.
, p. 2561 - 2573 (2007/10/03)
A number of benzimidazoles, having several substituents on the azole and benzene nuclei and C-2 (methylamino, ethylenediamine, morpholine, piperazine and piperidine) were prepared. Regioselective synthesis was designed for the N1-alkyl substituted benzimidazoles (14-15). X-Ray structure analysis of (14) was also revealed. Compounds were evaluated for their in vitro H1- antihistaminic activity in the isolated guinea-pig ileum method. The compound (11) exhibits best activity.
Synthesis of benzimidazole derivatives as antiallergic agents with 5- lipoxygenase inhibiting action
Nakano, Hiroyuki,Inoue, Tsutomu,Kawasaki, Nobuhide,Miyataka, Hideki,Matsumoto, Hitoshi,Taguchi, Takeo,Inagaki, Naoki,Nagai, Hiroichi,Satoh, Toshio
, p. 1573 - 1578 (2007/10/03)
Syntheses were conducted of novel benzimidazole derivatives that suppress histamine release from mast cells, inhibit 5-lipoxygenase, and possess antioxidative action. Among the compounds synthesized, 1-[2-[2-(4- hydroxy-2,3,5-trimethylphenoxy)ethoxy]ethyl]-2-(4-methyl-1- homopiperazino)benzimidazole (22) potently suppressed histamine release from rat peritoneal mast cells triggered by the antigen-antibody reaction, inhibited 5-lipoxygenase in rat basophilic leukemia-1 (RBL-1) cells, and prevented the NADPH-dependent lipid peroxidation induced by Fe3+-ADP in rat liver microsomes, in addition to an antagonizing the contraction of guinea pig ileum caused by histamine.