Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Mysore, India; Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Ootacamund 643 001, India(1).
Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Mysore, India; Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Ootacamund 643 001, India(1).
Bioorg Chem. 2014 Oct;56:27-33. doi: 10.1016/j.bioorg.2014.05.006. Epub 2014 May 24.
Herein, we report a library consisting of some novel glitazones containing thiazolidinedione and its bioisosteres, rhodanine and oxadiazolidine ring structures as their basic scaffold for their antidiabetic activity. Twelve novel glitazones with diverse chemical structures were designed and synthesized by adopting appropriate synthetic schemes and analyzed. Later, subjected to in vitro glucose uptake assay in the absence and presence of insulin to confirm their antidiabetic activity using rat hemi-diaphragm. The titled compounds exhibited glucose uptake activity ranging weak to significant activity. Compounds 4, 5, 9, 11, 15, 16, 19 and 20 showed considerable glucose uptake activity apart from rosiglitazone, a standard drug. Compound 16 happens to be the candidate compound from this study to investigate further. The illustration about their design, synthesis, analysis and glucose uptake activity is reported here along with the in vitro and in silico study based structure-activity relationships.
在此，我们报告了一个包含噻唑烷二酮及其生物等排体噻二唑和噁二唑环结构的新型格列酮库，作为其抗糖尿病活性的基本支架。通过采用适当的合成方案，设计并合成了 12 种具有不同化学结构的新型格列酮，并对其进行了分析。随后，在无胰岛素和有胰岛素的情况下进行体外葡萄糖摄取实验，以使用大鼠半膈肌来确认它们的抗糖尿病活性。这些标题化合物表现出弱至显著的葡萄糖摄取活性。除了标准药物罗格列酮外，化合物 4、5、9、11、15、16、19 和 20 还表现出相当的葡萄糖摄取活性。化合物 16 恰好是本研究中进一步研究的候选化合物。本文报道了它们的设计、合成、分析以及葡萄糖摄取活性，并结合基于结构-活性关系的体外和计算研究进行了说明。
