Quantitative Structure-Activity Relationships of H_1-Antihistaminic Benzimidazole Derivatives
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概要
- 論文の詳細を見る
The quantitative structure-activity relationships (QSAR) of 2-(4-substituted-1-piperazinyl)benzimidazole derivatives for antihistaminic activity were examined. Taking into consideration the specific conformations of some derivatives, a significant correlation was obtained using Verloop's STERIMOL parameters B_3 and L of the substituent at the 1-position of the benzimidazole nucleus. The results indicated that the derivatives having a substituent with a small breadth and an appropriate length at the 1-position showed potent activity. From the results, a model of the binding site is proposed. The QSAR of side effects (anticholinergic activity and central nervous system depressive effect) were also examined and the results showed that a sterically small substituent at the 1-position was required to decrease side effects.
- 公益社団法人日本薬学会の論文
- 1989-04-25
著者
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家村 隆一
Pharmaceuticals Research Center, Kanebo Ltd.,
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大高 博
Pharmaceuticals Research Center, Kanebo Ltd.,
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大高 博
New Drug Research Laboratories Kanebo Ltd.
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家村 隆一
Pharmaceuticals Research Center Kanebo Ltd.
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