Synthesis and In Vivo Acute Antihyperglycemic Evaluation of Novel Isosteviol Derivatives

Author(s): Junqing Chen, Xiaoming Zha, Min Sun, Jin Cai, Wen Zhou, Min Ji

Journal Name: Letters in Drug Design & Discovery

Volume 7 , Issue 9 , 2010

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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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Article Details

Year: 2010
Page: [686 - 693]
Pages: 8
DOI: 10.2174/157018010792929522
Price: $65

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