Grella G, Paglietti G, Sparatore F, Satta M, Manca P, Peana A
Istituto di Chimica Farmaceutica e Tossicologica, Università di Sassari.
Farmaco. 1992 Jan;47(1):21-35.
On the ground of the evidentiated choleretic activity of 3-[2-benzylbenzimidazol-1-yl]butanoic acid, 28 new acids were prepared in order to evaluate the influence of suitable substitutions in either C5 of heteroring or C3', C4', C5' of benzyl group in position 2 on the choleretic activity. Pharmacological results after i.v. administration of 0.5 mmol/Kg in rats confirmed a general high choleretic activity that in eleven cases showed during the first 4 hours an increase of bile volume higher than 80%, that is superior to that produced by dehydrocholic acid. Only in a few cases the bile volume increase was less than 37% of basal value.
基于3-[2-苄基苯并咪唑-1-基]丁酸已证实的利胆活性，制备了28种新的酸，以评估杂环C5位或2位苄基的C3'、C4'、C5'位上合适取代基对利胆活性的影响。大鼠静脉注射0.5 mmol/Kg后的药理结果证实了普遍较高的利胆活性，在11例中，在最初4小时内胆汁量增加高于80%，这优于去氢胆酸产生的效果。仅在少数情况下，胆汁量增加小于基础值的37%。
