Kabachnyĭ V I, Filippova L I, Drogovoz S M, Chernykh V P, Savchenko L G
Farmakol Toksikol. 1984 Jul-Aug;47(4):91-4.
Study of the choleretic activity of heterylamides of dicarboxylic acids has demonstrated that search for choleretic drugs in this series holds promise. The relationship of the choleretic activity and toxicity to the chemical structure of the compounds has been shown with special reference to 10 compounds--the derivatives of ethylene (ethane)-dicarboxylic acids. It has been discovered that the occurrence of the choleretic action is essentially determined by the presence in the structure of the compounds of a free cyrboxylic group. It has been also demonstrated that etherification or amidation of this group or hydrogenation of the unsaturated bond lead to the reduction or complete loss of the choleretic activity.
对二羧酸杂环酰胺的利胆活性研究表明,在该系列中寻找利胆药物是有前景的。特别参照10种化合物——乙烯(乙烷)-二羧酸的衍生物,已表明利胆活性和毒性与化合物化学结构之间的关系。已发现利胆作用的出现基本上取决于化合物结构中游离羧基的存在。还已证明,该基团的醚化或酰胺化或不饱和键的氢化会导致利胆活性降低或完全丧失。