简介：

简介：Gemfibrozilisawidelyusedlipidmodifyingdrugwithwell-establishedhypolipidemicandanti-atheroscleroticbenefits;however,thepresenceofacarboxylicacidmoietyinitsstructureisresponsibleforsideeffectsinthegastrointestinaltract.Theprincipleofbioisosterismwasappliedtodesignderivativesreplacingthecarboxylicacidgroup.Thecarboxylicacidgroupwasreplacedwithbioisotericgroups,suchas1,2,4-triazole-3-thiolandhydroxamicacid.Thederivativeswerethensynthesized,characterized,andevaluatedinratsforreducedgastrointestinalirritationandhypolipidemiceffects.Gemfibrozilwasusedasstandardforcomparison.Thederivativesdemonstratedlessgastricirritationandretainedhypolipidemiceffects,howeverthehypolipidemicaffectsweresignificantlylessthanthatofGemfibrozil.TheresultsofthisstudyoffersadirectionforfurtherresearchontheapplicationofbioisosterismforthedesignofnewderivativesofGemfibrozilandotherfibricacidderivatives.

简介：