新型吲哚-查尔酮类贝特类降脂药物的设计与合成
Design and synthesis of novel indole-chalcone fibrates as lipid lowering agents.
作者信息
Sashidhara Koneni V, Dodda Ranga Prasad, Sonkar Ravi, Palnati Gopala Reddy, Bhatia Gitika
机构信息
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, Uttar pradesh 226031, India.
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow, Uttar pradesh 226031, India.
出版信息
Eur J Med Chem. 2014 Jun 23;81:499-509. doi: 10.1016/j.ejmech.2014.04.085. Epub 2014 May 14.
A series of novel indole-chalcone fibrates were synthesized and their hypolipidemic activity was evaluated in triton WR-1339 induced hyperlipidemic rat model. Preliminary studies indicated that the hybrids 19, 24 and 29 exhibited potent in vitro antioxidant and significant in vivo antidyslipidemic effects. Our results suggest that these new hybrid architectures may serve as promising leads for the development of next generation lipid lowering agents.
合成了一系列新型吲哚-查尔酮纤维酸酯，并在 Triton WR-1339 诱导的高脂血症大鼠模型中评估了它们的降血脂活性。初步研究表明，化合物 19、24 和 29 表现出强大的体外抗氧化活性和显著的体内抗血脂异常作用。我们的结果表明，这些新的杂化结构可能成为开发下一代降脂药物的有前景的先导化合物。
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