2682-49-7, Name is Thiazolidin-2-one, belongs to thiazolidine compound, is a common compound. Computed Properties of C3H5NOSIn an article, once mentioned the new application about 2682-49-7.
Synthesis of new arylhydrazide bearing Schiff bases/thiazolidinone: alpha-Amylase, urease activities and their molecular docking studies
Alpha-amylase and urease enzyme over expression endorses various complications like rheumatoid arthritis, urinary tract infection, colon cancer, metabolic disorder, cardiovascular risk, and chronic kidney disease. To overcome these complications, we have synthesized new arylhydrazide bearing Schiff bases/thiazolidinone analogues as alpha-amylase and urease inhibitors. The analogues 1a-r were evaluated for alpha-amylase inhibitory potential. All analogues were found active and show IC50 value ranging between 0.8 ¡À 0.05 and 12.50 ¡À 0.5 muM as compare to standard acarbose (IC50 = 1.70 ¡À 0.10 muM). Among the synthesized analogs, compound 1j, 1r, 1k, 1e, 1b and 1f having IC50 values 0.8 ¡À 0.05, 0.9 ¡À 0.05, 1.00 ¡À 0.05, 1.10 ¡À 0.10, 1.20 ¡À 0.10 and 1.30 ¡À 0.10 muM respectively showed an excellent inhibitory potential. Analogs 2a-o were evaluated against urease activity. All analogues were found active and show IC50 value ranging between 4.10 ¡À 0.02 and 38.20 ¡À 1.10 muM as compare to standard thiourea (IC50 = 21.40 ¡À 0.21 muM). Among the synthesized analogs, compound 2k, 2a, 2h, 2j, 2f, 2e, 2g, 2b and 2l having IC50 values 4.10 ¡À 0.02, 4.60 ¡À 0.02, 4.70 ¡À 0.03, 5.40 ¡À 0.02, 6.70 ¡À 0.05, 8.30 ¡À 0.3, 11.20 ¡À 0.04, 16.90 ¡À 0.8 and 19.80 ¡À 0.60 muM respectively showed an excellent inhibitory potential. All compounds were characterized through 1H, 13C NMR and HR-EIMS analysis. Structure activity relationship of the synthesized analogs were recognized and confirmed through molecular docking studies.
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Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H419N | ChemSpider