Chaturvedi Devdutt, Ray Suprabhat, Srivastava Arvind K, Chander Ramesh
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, India.
Bioorg Med Chem. 2008 Mar 1;16(5):2489-98. doi: 10.1016/j.bmc.2007.11.062. Epub 2007 Nov 28.
omega-(2-Naphthyloxy) amino alkanes, obtained as major by-product during course of synthesis of carbamate esters from omega-(2-naphthyloxy) alkyl halides and amines, showed significant anti-hyperglycemic and lipid lowering activities in various test models as a novel class of compounds. Compounds were tested in rat GLM, SLM, STZ, and STZ-S models at 100mg/kg dose. Of these compound 13 was found to be the most active which caused lowering of sugar by 33.6%, 31.0%, 28.5%, and 73.8% in GLM, SLM, STZ, STZ-S, and db/db mice models, respectively. It also significantly effected lowering of LDL in rat model and also in Hamster model without reducing HDL. Most of the compounds showing anti-diabetic and lipid lowering activity have shown promising PPAR-alpha/gamma/delta-activity. Compounds 6, 13, and 19 have shown very good PPAR-alpha/gamma/delta activity.
ω-(2-萘氧基)氨基烷烃是由ω-(2-萘氧基)卤代烷与胺合成氨基甲酸酯的过程中得到的主要副产物，作为一类新型化合物，在各种测试模型中显示出显著的降血糖和降脂活性。化合物在大鼠GLM、SLM、STZ和STZ-S模型中以100mg/kg的剂量进行测试。其中化合物13被发现活性最高，在GLM、SLM、STZ、STZ-S和db/db小鼠模型中分别使血糖降低33.6%、31.0%、28.5%和73.8%。它还能显著降低大鼠模型和仓鼠模型中的低密度脂蛋白，且不降低高密度脂蛋白。大多数具有抗糖尿病和降脂活性的化合物显示出有前景的PPAR-α/γ/δ活性。化合物6、13和19显示出非常好的PPAR-α/γ/δ活性。
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