Synthesis and Structure-Activity Relationships of a New Series of Benzimidazoles as H_1-Antihistaminic Agents
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概要
- 論文の詳細を見る
New 2-(4-(4-azolybutyl)piperazinyl)-, 2-(4-(4-azolybutyl)piperazinylmethyl)-, 2-(4-(4-azolylbutyl)homopiperazinyl)- and 2-(4-(4-azolylbutyl)homopiperazinyl)methylbenzimidazoles were synthesized, characterized and tested for in vitro and in vivo H_1-antihistaminic activity. Structure-activity relationships impleid that the best antihistaminic activity required the simultaneous presence of a homopiperazinylbenzimidazole system (or a methylene linker between the benzimidazole and the piperazine rings) and an unsubstituted pyrazole ring. 1-(2-Ethoxyethyl)-2-{4-[4-(pyrazol-l-yl)butyl]homopiperazin-l-yl}benzimidazole (17), at its dimaleate salt, has been chosen for further development.
- 公益社団法人日本薬学会の論文
- 1997-08-15
著者
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Cuberes Maria
Department Of Medical Chemistry Laboratorios Dr.
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FRIGOLA Jordi
Departamento de Quimica Medica, Laboratorios Dr. Esteve
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Frigola Jordi
Department Of Medical Chemistry Laboratorios Dr.
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CONTIJOCH Montserrat
Department of Medical Chemistry, Laboratorios Dr.
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CALVET Carme
Department of Medical Chemistry, Laboratorios Dr.
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ALEGRE Julia
Department of Medical Chemistry, Laboratorios Dr.
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QUINTANA Jordi
Department of Medical Chemistry, Laboratorios Dr.
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Quintana Jordi
Department Of Medical Chemistry Laboratorios Dr.
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Calvet Carme
Department Of Medical Chemistry Laboratorios Dr.
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Alegre Julia
Department Of Medical Chemistry Laboratorios Dr.
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Contijoch Montserrat
Department Of Medical Chemistry Laboratorios Dr.
関連論文
- Heterocyclic Betaines. XXII. Azinium(Azolium) 4-Nitrobenzimidazolate Inner Salts and Their Derivatives with Several Interannular Spacers. Synthesis, Characterization and Antitrichomonal Activity
- Heterocyclic Betaines. XVI. Properties of (E)-1-Alkyl(or Aminoalkyl)-4-[2-(1H-benzimidazol-2-yl)vinyl]pyridinium Salts
- Synthesis and Structure-Activity Relationships of a New Series of Benzimidazoles as H_1-Antihistaminic Agents