Department of Chemistry, Mirpur University of Science & Technology (MUST), 10250, Mirpur (AJK), Pakistan.
Department of Chemistry & Biochemistry, Miami University 651, E. High Street, Oxford, 45056, Ohio, USA.
Future Med Chem. 2024;16(12):1255-1266. doi: 10.1080/17568919.2024.2342700. Epub 2024 May 10.
To synthesize novel more potent anti-diabetic agents. A simple cost effective synthetic strategy was used to synthesize 2-(2-arylidenehydrazinyl)thiazol-4(5)-ones. Fifteen new 2-(2-arylidenehydrazinyl)thiazol-4(5)-ones were established to check their anti-diabetic potential. From alpha(α)-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 α-amylase and anti-oxidant inhibition revealed that compounds are less active against α-amylase and anti-oxidant assays. 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.
为了合成新型强效抗糖尿病药物。采用简单且经济有效的合成策略，合成了 2-（2-芳亚甲基肼基）噻唑-4（5）-酮。建立了十五个新的 2-（2-芳亚甲基肼基）噻唑-4（5）-酮，以检查它们的抗糖尿病潜力。从α（α）-淀粉酶抑制、糖化抑制和抗氧化活性来看，大多数化合物都具有良好的抗糖尿病潜力。通过糖化抑制模式，发现所有测试的化合物都是更有效的抗糖尿病药物。α-淀粉酶和抗氧化抑制的结果表明，化合物对α-淀粉酶和抗氧化测定的活性较低。本研究得出结论，在芳环上引入各种吸电子基团并在噻唑啉核周围取代不同的官能团，有助于发现更好的抗糖尿病药物。
