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  • Title: Quantitative structure-activity relationships of H1-antihistaminic benzimidazole derivatives.
    Author: Iemura R, Ohtaka H.
    Journal: Chem Pharm Bull (Tokyo); 1989 Apr; 37(4):967-72. PubMed ID: 2569943.
    Abstract:
    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 B3 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.
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