New 1,2,3-Triazole-Tethered Thiazolidinedione Derivatives: Synthesis, Bioevaluation and Molecular Docking Study

被引:9
作者
Shaikh, Mubarak H. [1 ,2 ]
Subhedar, Dnyaneshwar D. [1 ]
Akolkar, Satish V. [1 ]
Nagargoje, Amol A. [1 ]
Asrondkar, Ashish [3 ]
Khedkar, Vijay M. [4 ]
Shingate, Bapurao B. [1 ]
机构
[1] Dr Babasaheb Ambedkar Marathwada Univ, Dept Chem, Aurangabad 431004, Maharashtra, India
[2] Radhabai Kale Mahila Mahavidyalaya, Dept Chem, Ahmednagar, Maharashtra, India
[3] Haffkine Inst Training Res & Testing, Mumbai, Maharashtra, India
[4] Vishwakarma Univ, Sch Pharm, Dept Pharmaceut Chem, Pune, Maharashtra, India
关键词
Click chemistry; 1; 2; 3-triazoles; anti-inflammatory activity; antioxidant activity; 4-thiazolidinedione; ACTIVATED RECEPTOR-GAMMA; FREE-RADICALS; ANTIMICROBIAL ACTIVITY; BIOLOGICAL EVALUATION; ACCURATE DOCKING; ANTIOXIDANT; GLIDE; CYTOTOXICITY; TRIAZOLES; DISCOVERY;
D O I
10.1080/10406638.2022.2069132
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
In search of new active molecules, a small focused library of 1,2,3-triazoles based 2,4-thiazolidinedione derivatives has been efficiently prepared via the click chemistry approach. Several derivatives were exhibited excellent anti-inflammatory activity compared to the standard drug. Further, the synthesized compounds were found to have potential antioxidant activity. Furthermore, to rationalize the observed biological activity data, the molecular docking study has also been carried out against the active site of inflammation enzyme PPAR gamma, which revealed a significant correlation between the binding score and biological activity for these compounds. The results of the in vitro and in silico study suggest that the triazole incorporated 2,4-thiazolidinedione derivatives may possess the ideal structural requirements for the further development of novel therapeutic agents.
引用
收藏
页码:3353 / 3379
页数:27
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