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Recent thiazolidinediones as antidiabetics

机译:噻唑烷二酮类药物最近作为抗糖尿病药

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Thiazolidinediones, a class of oral insulin sensitizing agents that improve insulin resistance, are agonists of peroxisome proliferator activated receptor-γ (PPAR-γ). Two clinically used drugs pioglitazone (ACTOS) and rosiglitazone (AVANDIA) have made a great contribution to therapy for type 2 diabetes. However, weight gain and hepatotoxicity are side effects of thiazolidinediones. For thiazolidinediones with lesser side effects, researchers are focusing on modification of side chain at C-5 of thiazolidinedione nucleus and its derivatization. Netoglitazone possesses both PPAR-α/γ dual agonistic activity. More thiazolidinedione derivatives like DRF-2189, PHT46, PMT13, DRF-2519 can be utilized as potent antidiabetic agents in future.
机译:噻唑烷二酮是一种改善胰岛素抵抗的口服胰岛素增敏剂,是过氧化物酶体增殖物激活受体-γ(PPAR-γ)的激动剂。两种临床使用的药物吡格列酮(ACTOS)和罗格列酮(AVANDIA)为2型糖尿病的治疗做出了巨大贡献。然而,体重增加和肝毒性是噻唑烷二酮类的副作用。对于具有较小副作用的噻唑烷二酮,研究人员集中在噻唑烷二酮核的C-5侧链的修饰及其衍生化上。耐格列酮同时具有PPAR-α/γ双重激动活性。将来,更多的噻唑烷二酮衍生物如DRF-2189,PHT46,PMT13,DRF-2519可用作有效的抗糖尿病药。

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