Synthesis and In Vivo Acute Antihyperglycemic Evaluation of Novel Isosteviol Derivatives
Isosteviol is a beyerane tetracyclic diterpenoid with a large variety of biological activities. In this article, a series of novel isosteviol derivatives containing the modification of C-18 carboxyl group (5-12), C-16 carbonyl group (14- 16) and heteroatom-containing frameworks fused with isosteviol structure (18-19) were synthesized and evaluated for their in vivo acute antihyperglycemeric effects. Among them, compound 8 exhibited the most potent antihyperglycemeric effects. Furthermore, primarily, structure-activity relationship (SAR) was also analyzed. The structures of all the newly synthesized compounds were determined by 1H, 13CNMR, MS, IR and elementary analysis.
Keywords: Isosteviol, Derivatives, Synthesis, Acute antihyperglycemeric, Antihyperglycemic, Isosteviol Derivatives, Beyerane tetracyclic diterpenoid, Antihyperglycemeric effects, Structure-activity relationship (SAR), Noncaloric sugar, Antitumor, Antihypertension, Anti-inflammatory, Glucocorticoid agonist, Antiproliferation, Anti-diabetic, Pharmacokinetic research, Glucuronic acid, Structure acitity relationship (SAR), (IVGTT), Antihyperglycemeric effect, Drug rosiglitazone maleate, Blood glucose level
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