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Study on the Synthesis of Novel PTP-1B Inhibitor Kinsenoside and Its Derivatives

Author: TangFei
Tutor: ZhangYongHui
School: Huazhong University of Science and Technology
Course: Medicinal Chemistry
Keywords: diabetes PTP PTP1B inhibitor Herba Anoectochili synthesis derivatives
CLC: R284.1
Type: Master's thesis
Year: 2010
Downloads: 82
Quote: 0
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Abstract


It remains a worldwide concern that type 2 diabetes mellitus is a metabolic disease for human health, so anti-diabetic drugs has been an important field in R&D of new drugs. Recently, it was found that type 2 diabetes attributes to some PTPs. Thereinto, protein tyosine phosphatase-1B(PTP-1B) negatively regulates insulinlike signal, in such, which is known as an important and potential target of type 2 diabetes.Our group has isolated kinsenoside from n-butanol extract from Anoectochilus roxburghii and has systematically studied its activity in STZ wistar rat and on enzymes related to type 2 diabetes. The results show that kinsenoside has significantly antihyperglycemic activity in animal, and kinsenoside has highly and selectively inhibitory action on PTP-1B, for lesser action on other homologous PTPs such as SHP, VHR and TCPTP et al.Based on the literatures, kinsenoside was designed and synthesized. Firstly, (R)-3-hydroxy-γ-butyrolactone was synthesized from starting material D-malic acid, and then connected with protected D-glucose with benzyl groups, finally kinsenoside was obtained after removal of protection groups. Our group designed some derivatives of kinsenoside in order to find some new compound with more active and higher selective inhibition on PTP-1B. One of them was synthesized using following procedure. Firstly, 2-benzyl-(R)-3-hydroxy-γ-butyrolactone was synthesized from (R)-3-hydroxy -γ-butyrolactone, and then connected with protected D-glucose by benzyl groups, finally KD1 was obtained after removal of protection groups.In addition, a few necessary intermediates have been synthesized, including 2-(4-fluorobenzyl)-(R)-3-hydroxy-γ-butyrolactone,2-Allyl-(R)-3-hydroxy-γ-butyrolacttone, and 2-methyl-(R)-3-hydroxy -γ-butyrolactone.

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