A novel route of one-pot multicomponent reaction of tosylates, aryl aldehydes and thiosemicarbazide for the synthesis of hydrazinyl thiazole is reported using Fe2O3 NPs derived from rust iron as a catalyst.

Sulfonylureas is being used throughout the world for the treatment of diabetes mellitus. The aim of the present study was to investigate mode of action of tosylacrylimidamide. Tosylacrylimidamide a non-classical bioisosteres of sulfonyl urea, bioisosteres refer to structurally distinct molecules eliciting a similar biological effect. In the present study we have determined the ability of tosylacrylimidamide to stimulate insulin secretion from MIN-6 cells. The compounds were tested in the presence of 5 mM glucose concentration, our results indicates that compound 4 e, 4 f, 4 g were the most effective insulin secretagogue's amongst reported, then 4 e, 4 f, 4 g were further evaluated at various concentration of compound keeping glucose concentration constant (5 mM), resulting 4 e showed 4.34 fold increase in insulin secretion at 1 mg/ml of compound, 4 f showed 7.4 fold increase in insulin secretion at 5 mg/ml of compound and 4 g has shown 7.6 fold increase in insulin secretion at 5 mg/ml of compound. The rest of the tosylacrylimidamide in our assay had only marginal effects on insulin secretion[a] S.

One-pot synthesis of highly substituted pyridines has been demonstrated via multicomponent reaction of aldehydes, malononitrile and thiophenol using Mg-Al hydrotalcite as a solid base and reusable catalyst. The catalytic activity is intimately connected to the basicity of the catalyst. The best activities were observed with the Mg/Al: 5 catalyst. The catalyst could be reused for further run without a significant loss in activity. The protocol was also applicable for various aromatic aldehydes which affords desired product in good to excellent yield.

A series of Novel Methylsulfonylacrylimidamide analogs (4a – 4h) were designed, synthesized, and screened for their α-glucosidase inhibitory activity. The results indicated that some of the synthesized derivatives displayed inhibitory activities against α-glucosidase with IC50 values ranging from 10.35 ± 0.15 to 60.39 ± 1.77 µM when compared to standard drug acarbose (IC50 832.22 ± 2.00 µM). Among the synthesized derivatives, compounds 4f & 4h with a dicyclohexyl and dioctyl substitution in the acrylimidamide displayed the most significant inhibitory activity with the IC50 value of 14.54 ± 0.19 µM and 10.35 ± 0.15 µM. The inhibitory action of compounds 4f and 4h against α-glucosidase was studied by enzyme kinetic and molecular docking. In vitro, cytotoxicity showed that 4f and 4h exhibited low cytotoxicity against human cell lines. The ADME study suggested that most compounds will likely be orally active as they obeyed Lipinski's rule of five. Our studies showed that these derivatives could be considered a new class of α-glucosidase inhibitors.