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4-Thiazolidones: Centenarian History, Current Status and Perspectives for Modern Organic and Medicinal Chemistry

机译:4-噻唑烷酮:百年历史,现代有机药物化学的现状和展望

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摘要

The potential of 4-thiazolidones (2,4-thiazolidinediones, 2-thioxo(imino)-4-thiazolidones) as drugs is under consideration by the pharmaceutical science since the beginning of the XX century. During recent years a new phase has been seen in this field. Centerarian history of synthetic research possibilities of these heterocycles lead to diversity in modelling biologically active compounds using 4-thiazolidone scaffolds. Modification of the 4- thiazolidone cycle on 2-, 3-, 4- or 5-position is successful to achieve synthetic products with a wide spectrum of pharmacological activity and has received considerable attention in this review. Currently 4-thiazolidones are considered as a new class of antidiabetic (insulin-sensitising) drugs and potent aldose reductase inhibitors, which possess potential for the treatment of diabetes complications (cataract, nephropathy, neuropathy). Novel 4- thiazolidones are undergoing different stages of clinical trials as potential thyromimetic, antimicrobial, antiviral, anti-ischaermic, cardiovascular, anticancer drugs.
机译:自二十世纪初以来,药学界一直在考虑4-噻唑烷酮(2,4-噻唑烷二酮,2-硫代(亚氨基)-4-噻唑烷酮)作为药物的潜力。近年来,在该领域出现了一个新阶段。这些杂环的合成研究可能性的中心历史导致了使用4-噻唑烷酮支架对生物活性化合物进行建模的多样性。在2-,3-,4-或5-位上修饰4-噻唑烷酮循环可成功获得具有广泛药理活性的合成产品,并且在本综述中受到了广泛关注。目前,4-噻唑烷酮被认为是一类新型的抗糖尿病(胰岛素敏感性)药物和有效的醛糖还原酶抑制剂,它们具有治疗糖尿病并发症(白内障,肾病,神经病)的潜力。新型的4-噻唑烷酮类药物正在经历不同的临床试验阶段,包括潜在的促甲状腺激素药,抗微生物药,抗病毒药,抗缺血药,心血管药,抗癌药。

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