Synthesis of Dynamic 2-Ethoxycarbonyl-4H-3, 1-Benzoxazin-4-one and its Behavior Towards Nitrogen Nucleophiles

The behavior of  2-ethoxycarbonyl-4H-3,1-benzoxazin-4-one and its behavior towards nitrogen nucleophiles namely, hydrazine hydrate, formamide, benzylamine, ethylamine, piperidine, ethanol amine, o-phenylenediamine, and glucosamine hydrochloride has been investigated. Also the reaction of 3-[aminoquinazolin-4(3H)-one-2-yl]formic acid hydrazide with aromatic aldehydes and phenylisothiocyanate has been discussed. The structure of the prepared compounds are elucidated using physical and spectral data like, FT-IR, 1HNMR, and mass spectroscopy

Synthesis of bioactive quinazolin-4(3H)-one derivatives via microwave activation tailored by phase-transfer catalysis

A series of nine new 2,3-disubstituted 4(3H)-quinazolin-4-one derivatives was furnished starting from the 2-propyl-4(3H)-quinazoline-4-one (2). The reinvestigation of the key starting quinazolinone 2 was performed under microwave irradiation (MW) and solvent-free conditions. Combination of MW and phase-transfer catalysis using tetrabutylammonium benzoate (TBAB) as a novel neutral ionic catalyst was used for carrying out N-alkylation and condensation reactions of compound 2 as a simple, efficient and eco-friendly technique. The structure of the synthesized compounds was elucidated using different spectral and chemical analyses. In vitro antimicrobial activity of the compounds was investigated against four bacterial and two fungal strains; very modest activity was achieved. Some of the synthesized compounds were screened for their antitumor activity against different human tumor cell lines. The screened compounds exhibited a significant antitumor activity on some of the cancer cell lines, melanoma (SK-MEL-2), ovarian cancer (IGROV1), renal cancer (TK-10), prostate cancer (PC-3), breast cancer (MCF7) and colon cancer (HT29). The most active, even more active than the reference 5-fluorouracil, were found to be ethyl 4-[(4-oxo-2-propylquinazolin-3(4H)-yl)methyl]benzoate (3c), 3-{2-[6-(pyrrolidin-1-yl-sulfonyl)-1,2,3,4-tetrahydroquinoline]-2-oxoethyl}-2-propylquinazolin-4(3H)-one (3e), N’-[(E)-(2H-1,3-benzodioxo-5-yl)methylidene]-2-(4-oxo-2-propylquinazolin-3(4H)-yl)acetohydrazide (10a), N’-[(E)-(4-hydroxyphenyl)methylidene]-2-(4-oxo-2-propylquinazo-lin-3(4H)-yl)acetohydrazide (10b) and N’-[(E)-(4-nitrophenyl)methylidene]-2-(4-oxo-2-propylquinazolin-3(4H)-yl)acetohydrazide (10c)

Determination of the tensile properties and biodegradability of cornstarch-based biopolymers plasticized with sorbitol and glycerol

In this study, the effects of various quantities of sorbitol and glycerol plasticizers (0%, 30%, 45%, and 60%) on cornstarch-based film were examined to develop a novel polymer for usage with biodegradable materials. The film was prepared using the casting process. According to the test findings, the application of the plasticizer concentrations affected the thickness, moisture content, and water absorption of the film. When plasticizer concentrations were increased to 60%, the tensile stress and Young’s modulus of plasticized films dropped regardless of plasticizer type. However, the thin film with addition of 30% sorbitol plasticizer demonstrated a steady value of Young’s modulus (60.17 MPa) with an increase in tensile strength (13.61 MPa) of 46%, while the lowest combination of tensile strength and Young’s modulus is the film that was plasticized with 60% glycerol, with 2.33 MPa and 16.23 MPa, respectively. In summary, the properties and performance of cornstarch-based film were greatly influenced by plasticizer types and concentrations. The finest set of features in this research appeared in the film plasticized with 30% sorbitol, which achieved the best mechanical properties for food packaging applications

Ginger (Zingiber Officinale)-derived nanoparticles in Schistosoma mansoni infected mice: Hepatoprotective and enhancer of etiological treatment.

BackgroundNanotechnology has been manufactured from medicinal plants to develop safe, and effective antischistosmal alternatives to replace today's therapies. The aim of the study is to evaluate the prophylactic effect of ginger-derived nanoparticles (GNPs), and the therapeutic effect of ginger aqueous extract, and GNPs on Schistosoma mansoni (S. mansoni) infected mice compared to praziquantel (PZQ), and mefloquine (MFQ).Methodology/principal findingsEighty four mice, divided into nine different groups, were sacrificed at 6th, 8th, and 10th week post-infection (PI), with assessment of parasitological, histopathological, and oxidative stress parameters, and scanning the worms by electron microscope. As a prophylactic drug, GNPs showed slight reduction in worm burden, egg density, and granuloma size and number. As a therapeutic drug, GNPs significantly reduced worm burden (59.9%), tissue egg load (64.9%), granuloma size, and number at 10th week PI, and altered adult worm tegumental architecture, added to antioxidant effect. Interestingly, combination of GNPs with PZQ or MFQ gave almost similar or sometimes better curative effects as obtained with each drug separately. The highest therapeutic effect was obtained when ½ dose GNPs combined with ½ dose MFQ which achieved 100% reduction in both the total worm burden, and ova tissue density as early as the 6th week PI, with absence of detected eggs or tissue granuloma, and preservation of liver architecture.Conclusions/significanceGNPs have a schistosomicidal, antioxidant, and hepatoprotective role. GNPs have a strong synergistic effect when combined with etiological treatments (PZQ or MFQ), and significantly reduced therapeutic doses by 50%, which may mitigate side effects and resistance to etiological drugs, a hypothesis requiring further research. We recommend extending this study to humans

<span style="mso-ansi-language:EN-GB" lang="EN-GB">Synthesis and behaviour of 2-(furan-2-yl)vinyl-4<i style="mso-bidi-font-style:normal">H</i>-3,1-benzoxazin-4-one towards nitrogen and carbon nucleophiles </span>

1574-1583A convenient new procedure for the synthesis of 2-(furan-2-yl)vinyl-4<i style="mso-bidi-font-style: normal">H-3,1-benzoxazin-4-one 4 is reported. Reaction of the respective benzoxazinone with various nitrogen nucleophiles affords 3-substituted quinazolinone and benzamide derivatives. Benzoxazinone 4 is converted to 4(3H)-quinazolinone followed by acylation, chlorination, and alkylation, which also is catalytically hydrogenated

Synthesis, Characterization and Evaluation of Supercapacitive Response of Dodecylbenzenesulphonic Acid (DBSA) Doped Polypyrrole/Zirconium Dioxide Composites

An in-situ chemical oxidative method was used to effectively synthesize a promising supercapacitor material based on PPy/ZrO2 composites. The synthesized materials were characterized by different analytical techniques, such as UV/visible (UV/Vis) spectroscopy, Fourier-transform infra-red spectroscopy (FTIR), X-ray diffraction (XRD), thermogravimetric analysis (TGA), and scanning electron microscopy (SEM). The inclusion of ZrO2 into the PPy matrix was verified by vibrational spectra and structural analyses. The (TGA) results showed that incorporating ZrO2 into the polymeric matrix improved its thermal stability. In addition, the electrochemical properties of the synthesizedmaterials were investigated byusing cyclic voltammetry (CV) and galvanostatic charge/discharge (GCD). The PPy/ZrO2 composite demonstrated excellent super capacitive performance, and high specific capacity of 337.83 F/g, with an exceedingly high energy density of 187.68 Wh/kg at a power density of 1000 W/kg. The composite materials maintain good stability after 1000 charge and discharge cycles, with 85% capacitance retention. The PPy/ZrO2 possesses a high capacitance, an attractive micro-morphology, and a simple synthesis method. The findings indicate that the PPy/ZrO2 composite could be a promising electrode material for high-performance supercapacitor applications

Determination of the Tensile Properties and Biodegradability of Cornstarch-Based Biopolymers Plasticized with Sorbitol and Glycerol

In this study, the effects of various quantities of sorbitol and glycerol plasticizers (0%, 30%, 45%, and 60%) on cornstarch-based film were examined to develop a novel polymer for usage with biodegradable materials. The film was prepared using the casting process. According to the test findings, the application of the plasticizer concentrations affected the thickness, moisture content, and water absorption of the film. When plasticizer concentrations were increased to 60%, the tensile stress and Young’s modulus of plasticized films dropped regardless of plasticizer type. However, the thin film with addition of 30% sorbitol plasticizer demonstrated a steady value of Young’s modulus (60.17 MPa) with an increase in tensile strength (13.61 MPa) of 46%, while the lowest combination of tensile strength and Young’s modulus is the film that was plasticized with 60% glycerol, with 2.33 MPa and 16.23 MPa, respectively. In summary, the properties and performance of cornstarch-based film were greatly influenced by plasticizer types and concentrations. The finest set of features in this research appeared in the film plasticized with 30% sorbitol, which achieved the best mechanical properties for food packaging applications