Synthesis, anti-diabetic profiling and molecular docking studies of 2-(2-arylidenehydrazinyl)thiazol-4(5H)-ones

被引：4
作者：
Mehmood, Hasnain [1 ]
Haroon, Muhammad [2 ]
Akhtar, Tashfeen [1 ]
Woodward, Simon [3 ]
Haq, Saadia [4 ,5 ]
Alshehri, Saad M. [6 ]
机构：
[1] Mirpur Univ Sci & Technol, Dept Chem, Mirpur 10250, Ajk, Pakistan
[2] Miami Univ, Dept Chem & Biochem, 651 E High St, Oxford, OH 45056 USA
[3] GSK, Carbon Neutral Labs Sustainable Chem, Univ Pk, Nottingham NG7 2RD, England
[4] Khwaja Fareed Univ Engn & Informat Technol, Inst Chem, Rahim Yar Khan 64200, Pakistan
[5] Khwaja Fareed Univ Engn & Informat Technol, Ctr Theoret & Computat Res, Rahim Yar Khan 64200, Pakistan
[6] King Saud Univ, Coll Sci, Dept Chem, Riyadh 11451, Saudi Arabia
来源：
FUTURE MEDICINAL CHEMISTRY | 2024年 / 16卷 / 12期
关键词：
anti-diabetic; cyto-toxicity; HRMS; molecular docking; NMR; SAR; thiazol-4(5H)-ones; PANCREATIC ALPHA-AMYLASE; BIOLOGICAL EVALUATION; DERIVATIVES; POTENT; INHIBITORS; DESIGN; BINDING;
D O I：
10.1080/17568919.2024.2342700
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Aim: To synthesize novel more potent anti-diabetic agents. Methodology: A simple cost effective Hantzsch's synthetic strategy was used to synthesize 2-(2-arylidenehydrazinyl)thiazol-4(5H)-ones. Results: Fifteen new 2-(2-arylidenehydrazinyl)thiazol-4(5H)-ones were established to check their anti-diabetic potential. From alpha(alpha)-amylase inhibition, anti-glycation and anti-oxidant activities it is revealed that most of the compounds possess good anti-diabetic potential. All tested compounds were found to be more potent anti-diabetic agents via anti-glycation mode. The results of alpha-amylase and anti-oxidant inhibition revealed that compounds are less active against alpha-amylase and anti-oxidant assays. Conclusion: This study concludes that introduction of various electron withdrawing groups at the aryl ring and substitution of different functionalities around thiazolone nucleus could help to find out better anti-diabetic drug.
引用
收藏
页码：1255 / 1266
页数：12
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