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.
The current manuscript elucidates Ficus benghalensis (F.B.) leaf extract‐mediated green synthesis of Fe3O4 nanoparticles as magnetic support for the synthesis of novel Fe3O4@Ag‐S‐CH2‐COOH magnetic nanocomposite. The structure of Fe3O4@Ag‐S‐CH2‐COOH is confirmed by various characterization techniques such as FT‐IR, XRD, SEM, HR‐TEM, BET, and VSM analyses. Catalytic potential of Fe3O4@Ag‐S‐CH2‐COOH was tested for the syntheses of novel 3,4‐dihydropyrimidin‐2(1H)‐ones through one‐pot Biginelli reaction of aryl aldehydes, urea, and avobenzone. The Fe3O4@Ag‐S‐CH2‐COOH exhibited outstanding catalytic activity towards Biginelli reaction and could be easily separated from the reaction mixture by an external magnet. Interestingly, catalyst could be recycled for four successive turns without considerable loss in the catalytic activity. The structure of novel 3,4‐dihydropyrimidin‐2(1H)‐ones were confirmed by FT‐IR, 1H, 13C‐NMR, mass spectrometry, and single crystal X‐ray diffraction technique. Synthesized novel 3,4‐dihydropyrimidin‐2(1H)‐ones were tested for anti‐cancer activity against human liver cancer cell line Hep‐G2 along with anti‐angiogenesis study and confirmed by molecular docking investigations.
The ongoing work describes the catalytic evaluation of γ‐Fe2O3@Ag‐S‐CH2‐COOH magnetic nanoparticles utilizing γ‐Fe2O3 obtained from waste iron rust for one‐pot synthesis of 2,3‐dihydroquinazolin‐4(1H)‐ones. As‐prepared γ‐Fe2O3@Ag‐S‐CH2‐COOH nanoparticles were characterized by Fourier transform infrared spectroscopy (FT‐IR), X‐ray diffraction (XRD), scanning electron microscopy (SEM), energy‐dispersive X‐ray spectroscopy (EDX), dynamic light scattering (DLS), transmission electron microscopy (TEM), X‐ray photoelectron spectroscopy (XPS), and Brunauer–Emmett–Teller (BET) technique. The catalytic performance of greener γ‐Fe2O3@Ag‐S‐CH2‐COOH nanoparticles was utilized in the synthesis of 2,3‐dihydroquinazolin‐4(1H)‐ones. The excellent catalytic performance was shown by magnetic nanoparticles in addition to its ease of separation by an external magnet and can be recycled for five consecutive turns without significant loss of catalytic activity. Furthermore, the synthesized 2,3‐dihydroquinazolin‐4(1H)‐ones were confirmed by FT‐IR, 1H, 13C nuclear magnetic resonance (NMR), and mass spectrometry. Moreover, the synthesized 2,3‐dihydroquinazolin‐4(1H)‐ones were evaluated for their anticancer efficiency against the human skin cancer cell line B16F10 along with molecular docking investigation.
A simple method for synthesis of Schiff bases, from o-hydroxy benzaldehyde and substituted aromatic primary amines dissolved in ethyl alcohol, under microwave irradiation is reported. The remarkable advantages of this method are simple experimental procedure, short reaction time with pure product and excellent yield. Synthesized compounds were tested for antibacterial activity.
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