Synthesis, characterization and biological evaluation of some novel 2,4-thiazolidinediones as potential cytotoxic, antimicrobial and antihyperglycemic agents
作者:Vasudeva Rao Avupati、Rajendra Prasad Yejella、Annapurna Akula、Girija Sankar Guntuku、Bhagya Raju Doddi、Venkata Rao Vutla、Suvarna Ratna Anagani、Lakshmana Santhi Adimulam、Aruna Kumar Vyricharla
DOI:10.1016/j.bmcl.2012.08.052
日期:2012.10
A series of some novel 2,4-thiazolidinediones (TZDs) (2a–x) have been synthesized and characterized by FTIR, 1H NMR, 13C NMR and LC mass spectral analysis. All the synthesized compounds were evaluated for their cytotoxicity, antimicrobial and in vivo antihyperglycemic activities. Among the tested compounds for cytotoxicity using Brine Shrimp Lethality assay, compound 2t ((Z)-5-(4-((E)-3-oxo-3-(thi
合成了一系列新颖的2,4-噻唑烷二酮(TZDs)(2a – x),并通过FTIR,1 H NMR,13 C NMR和LC质谱分析对其进行了表征。评价所有合成的化合物的细胞毒性,抗微生物和体内抗高血糖活性。在使用盐水虾致死性测定法测试的细胞毒性化合物中,化合物2t((Z)-5-(4-((E)-3-oxo-3-(噻吩-2-基)丙-1-烯基)亚苄基) -1,3-噻唑烷-2,4-二酮)在ED 50值为4.00±0.25μg/ mL时表现出显着的抑制活性,并且该活性水平与含ED 50的参比药物鬼臼毒素相当值3.61±0.17μg/ mL。使用琼脂井扩散分析法筛选对所选革兰氏阳性,革兰氏阴性和真菌菌株的抗菌活性,并以μg/ mL的最小抑菌浓度(MIC)表示活性。从化合物2s((Z)-5-(4-((E)-3-(3,5-双(苄氧基)苯基)-3-氧代丙-1-烯基)亚苄基)-1的抗菌活性的结果,发现3-噻唑烷-2