Synthesis and hypoglycemic activity evaluation of rhein amide derivatives

In order to investigate the relationship of the structure and hypoglycemic activity, rhein amide derivatives 2a – 2e were synthesized and their hypoglycemic activities were evaluated by glucose consumption in HepG2. Their structures were characterized by 1 H-, 13 C NMR, IR, mass and elemental analys...

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Published inMedicinal chemistry research Vol. 22; no. 5; pp. 2228 - 2234
Main Authors Zhu, Xiaokang, Ye, Xiaoli, Song, Liu, Luo, Yonghuang, Tang, Qing, Jin, Yanan, Li, Xuegang
Format Journal Article
LanguageEnglish
Published New York Springer-Verlag 01.05.2013
Subjects
Biochemistry
Biomedical and Life Sciences
Biomedicine
Cell Biology
Original Research
Pharmacology/Toxicology
Hypoglycemic activity
Glucose consumption
Rhein derivatives
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Summary:In order to investigate the relationship of the structure and hypoglycemic activity, rhein amide derivatives 2a – 2e were synthesized and their hypoglycemic activities were evaluated by glucose consumption in HepG2. Their structures were characterized by 1 H-, 13 C NMR, IR, mass and elemental analysis. All the compounds exhibited strong hypoglycemic activity in improving glucose consumption in HepG2 cell assays in vitro, which was influenced by the diversity of rhein amide derivatives. The compounds 2a – c , 2f , and 2g bearing heterocyclic ring were proved to be more potentially useful in glucose consumption than dimethyldiguanide. Among all the compounds, compound 2f exhibited the strongest activity on glucose consumption, while compound 2d showed the weakest activity.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-012-0215-7