Concurrent construction of five and six membered fused N-heretocyclic ring was achieved via a conceptually new three-component reaction affording 6,6a-dihydroisoindolo[2,1-a]quinazoline-5,11-diones as novel inhibitors of TNF-αin vitro. This represents one of the few examples of direct TNF-α inhibition by small molecules.
A one-pot Yb(III)-mediated cascade reaction has been developed leading to small molecules based on a novel structural motif, i.e. quinazolin-4-one moiety fused with an isoquinoline ring, for potential inhibition of TNF-α.
The first example of an intramolecular decarboxylative acylation reaction for the synthesis of 4H‐benzoxazin‐4‐one derivatives has been described. The silver‐mediated reaction has a broad substrate scope and provides a mild and rapid approach to the corresponding products in high yields.
A one-pot cascade reaction has been developed leading to the concurrent construction of six and five membered fused N-heterocyclic rings of indazolo[3,2-b]quinazolinones. The methodology involved the reaction of isatoic anhydride, a hydrazine and o-iodo benzaldehyde in the presence of Pd(PPh(3))(4) and BINAP in MeCN. The mechanism of this cascade reaction is discussed. A variety of indazolo[3,2-b]quinazolinone derivatives were prepared by using this methodology in good yields, some of which were tested for their PDE4 inhibitory properties in vitro. The dose response and docking study performed using a representative compound is presented.
This work uses Psidium guajava leaf extracts to easily and quickly synthesise Cerium nanoparticles (Ce NPs) and Zn: CeO2 NPs (Zn-Ce NPs) (PGE). The generated G - CeO2 and Zn: CeO2 NPs were examined using X-ray diffraction (XRD), Energy Dispersive Analysis of X-Ray (EDAX), Fourier transformed infrared spectroscopy (FT-IR), UV-Visible spectroscopy (UV-Vis), and Scanning Electron Microscopy (SEM) techniques. The presence of OH, -NH2, and C=O groups, which were essential for the synthesis of G-CeO2 and Zn: CeO2 NPs, was detected by FT-IR spectroscopy. The XRD analysis supports the fluorite cubic structure of the resulting particles for G-CeO2 and Zn: CeO2 NPs. The findings of the elemental analysis by EDX demonstrated that the doping effects of Zn2+ in G-CeO2 NPs effectively enhanced the percentages of cerium and oxygen. G-CeO2 and Zn: CeO2 nanoparticles were evenly dispersed, and a SEM microscopic investigation also revealed that the produced nanoparticles were spherical in shape. Both the G-CeO2 and Zn: CeO2 nanoparticles demonstrated effective antibacterial and antifungal properties. To measure photocatalytic activity, the degradation of methylene blue (MB) in aqueous solution under visible light irradiation was utilised. The findings demonstrated that Zn doping considerably increased Ce NPs' photocatalytic activity. Using Zn dopant, it has been discovered that the optical band gap of Ce NPs has decreased from 3.69 eV to 3.55 eV. Both the G-CeO2 and Zn: CeO2 nanoparticles demonstrated effective antibacterial and antifungal properties. By increasing the concentration of both G-CeO2 and Zn: CeO2 NPs, the viability of the cancer cells L929 and HCT 116 was partly reduced.
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