Synthesis and Antibacterial Activity of 3-(Substituted)-2-(4-oxo-2-phenylquinazolin-3(4H)-ylamino)quinazolin-4(3H)-one

Appani, Ramgopal; Bhukya, Babu Rao; Gangarapu, Kiran

doi:10.1155/2016/1249201

Cited by 7 publications

(7 citation statements)

References 18 publications

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“…The biological activities of PHB, PHB–diol, PHB–diacrylate, and PHB–thiol polymers (PI–PVI) were tested against some Gram‐positive bacteria, including Staphylococcus aureus, and some Gram‐negative bacteria, including Escherichia coli , Klebsiella pneumoniae , and Pseudomonas aeruginosa, with the standard drug ciprofloxacin with the agar cup plate method (Table ) . PHB, PHB–diol, PIV, and PI displayed great inhibition zones on E. coli .…”

Section: Resultsmentioning

confidence: 99%

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Functionalization of poly(3‐hydroxybutyrate) with different thiol compounds inhibits MDM2–p53 interactions in MCF7 cells

Abdelwahab

El‐Barbary

El-Said

et al. 2018

J of Applied Polymer Sci

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High-molecular-weight poly(3-hydroxybutyrate) (PHB) has a low reactivity toward its terminal functional groups. Thus, the chemical reactivity of PHB was enhanced by the chemical degradation that occurred via β-elimination through the functionalization of PHB with ethylene glycol to give a low-molecular-weight PHB-diol. The reaction of PHB-diol with acryloyl chloride gave PHB-diacrylate, which was grafted by thiol compounds, such as ethane dithiol, 2-mercaptoethanol, ethane thiol, dithiothreitol, butane thiol, and thioglycolic acid, via a Michael-type addition reaction. The chemical and thermal properties of the functionalized PHB-thiol products were characterized with Fourier transform infrared spectroscopy, 1 H-NMR, gel permeation chromatography, differential scanning calorimetry, and thermogravimetric analysis techniques. X-ray diffraction showed that the PHB-thiol polymers had slight differences in crystallinity compared with neat PHB. The biological activities of the neat polymer and new PHB-thiol polymers, including the antibacterial and anticancer activities, were tested, and some of these products showed antibacterial and anticancer activities. These anticancer activities were attributed to the ability of these PHB-thiol polymers to induce apoptosis (as revealed by the higher expression of Bax and caspase 9 and the lower expression of Bcl2) and cell-cycle arrest in the G0/G1 phase, which is associated with the higher expression of p53 and p21 and the lower expression of the p53 inhibitor, MDM2. Thus, the anticancer effect of these PHB-thiol polymers may have been due to their ability to inhibit MDM2-p53 interactions.

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Section: Resultsmentioning

confidence: 99%

“…The antibacterial activities of the polymers were assessed via the detection of the inhibition zones with the agar cup plate method, as previously described …”

Section: Methodsmentioning

confidence: 99%

Functionalization of poly(3‐hydroxybutyrate) with different thiol compounds inhibits MDM2–p53 interactions in MCF7 cells

Abdelwahab

El‐Barbary

El-Said

et al. 2018

J of Applied Polymer Sci

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“…The zone of inhibition was measured by the agar diffusion method. 56 The nutrient agar media were prepared, sterilized, and poured into sterile Petri dishes. Media were allowed to solidify, and then the bacteria were inoculated from the cultivated bacterial suspension with the aid of the swapping method followed by boring in the plate with the aid of a cork-borer to achieve a certain size of the cavity.…”

Section: Methodsmentioning

confidence: 99%

Aniline-co-o-anthranilic Acid Copolymer-Chitosan/Ag@AgCl Nanohybrid as a Carrier for (E)-N′-(Pyridin-2-ylmethylene) Hydrazinecarbothiohydrazide Release and Antimicrobial Activity

et al. 2021

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Poly(aniline- co - o -anthranilic acid)-chitosan/silver@silver chloride (PAAN-CS/Ag@AgCl) nanohybrids were synthesized using different ratios of Ag@AgCl through a facile one-step process. The presence of CS led to the formation of the nanohybrid structure and prevented the aggregation of the copolymer efficiently. The synthesized nanohybrids were fully characterized by transmission electron microscopy, X-ray diffraction, Fourier transform infrared (FTIR) spectroscopy, and thermogravimetric analysis. ( E )- N ′-(Pyridin-2-ylmethylene) hydrazinecarbothiohydrazide I was prepared using thiosemicarbazide and confirmed by 1 H-NMR, 13 C-NMR, and FTIR analyses. Loading of the azine derivative I using various concentrations at different pH values onto the nanohybrid was followed by UV–vis spectroscopy. Langmuir and Freundlich adsorption isotherm models were used to describe the equilibrium isotherm, and the adsorption followed the Langmuir adsorption isotherm. A pseudo-second-order model was used to describe the kinetic data. A PAAN-CS/Ag@AgCl nanohybrid loaded with azine I interestingly showed efficient antimicrobial activity against Escherichia coli and Staphylococcus aureus more than the azine derivative I . The release of azine I at different pH values (2–7.4) was investigated and the kinetics of release were studied using zero-order, first-order, second-order, Higuchi, Hixson–Crowell, and Korsmeyer–Peppas equations.

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“…Using polymeric nanoparticles and nanocomposites as controlled drug delivery systems have attracted great attention due to their high drug loading capacity and ability to release the loaded drug in controlled fashion [22]. Table 2 and Figure 7 showed the antibacterial activity against some Gram-positive and Gram-negative bacteria using agar cup plate method, ciprofloxacin was used as standard drug [23]. Compound PVTQ, copolymers PSco-PPVTQ, PMMA-co-PPVTQ, PS-co-PAPQ and PMMA-co-PAPQ showed a negative inhibition zones towards all types of bacteria under study.…”

Section: Antibacterial Activitymentioning

confidence: 99%

Copolymerization of Quinazolinone Derivatives With Styrene, Methyl Methacrylate and Their Silver Nanocomposites for Biological Applications

El-Said¹,

El‐Barbary²,

ElKholy³

et al. 2021

Preprint

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Reaction of 2-mercapto-3-phenylquinazolin-4(3H)-one (MPQ) with both 4-vinyl benzyl chloride and allyl bromide furnished the reactive heterocyclic monomers 3-phenyl-2-((4-vinylbenzyl) thio) quinazolin-4(3H)-one (PVTQ) and 2-(allylthio)-3-phenylquinazolin-4(3H)-one (APQ), respectively. Copolymerization of PVTQ monomer with styrene and methyl methacrylate in the presence of 2,2′-azobisisobutyronitrile (AIBN) afforded the copolymers PS-co-PPVTQ and PMMA-co-PPVTQ, respectively. Similarly, copolymerization of monomer APQ with styrene and methyl methacrylate (MMA) afforded the copolymers PS-co-PAPQ and PMMA-co-PAPQ, respectively. The resulted copolymers were characterized by using FT-IR, 1H-NMR and GPC techniques. Silver nanocomposites of PS, PMMA, PS-co-PPVTQ, PMMA-co-PPVTQ, PS-co-PAPQ and PMMA-co-PAPQ were synthesized by the addition of silver nitrate into the polymer solution. The reduction of silver ions into silver nanoparticles was performed in DMF and water. Thermogravimetric (TGA) analysis was used to determine the thermal stability of the copolymers and their silver nanocomposites. The X-ray diffraction (XRD) analysis indicated the amorphous structures of the co-polymers and confirmed the formation of silver nanoparticles. The antitumor and antibacterial activities were screened for the copolymers and enhanced by the formation of their silver nanocomposites. In vivo antitumor activity in Ehrlich Ascitic Carcinoma (EAC) mice model showed that PS-co-PPVTQ/Ag NPs, PMMA-co-PPVTQ/Ag NPs, and PMMA-co-PAPQ/Ag NPs displayed promising inhibitory effects against EAC and induce apoptosis against MCF-7 cells.

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Synthesis and Antibacterial Activity of 3-(Substituted)-2-(4-oxo-2-phenylquinazolin-3(4H)-ylamino)quinazolin-4(3H)-one

Cited by 7 publications

References 18 publications

Functionalization of poly(3‐hydroxybutyrate) with different thiol compounds inhibits MDM2–p53 interactions in MCF7 cells

Functionalization of poly(3‐hydroxybutyrate) with different thiol compounds inhibits MDM2–p53 interactions in MCF7 cells

Aniline-co-o-anthranilic Acid Copolymer-Chitosan/Ag@AgCl Nanohybrid as a Carrier for (E)-N′-(Pyridin-2-ylmethylene) Hydrazinecarbothiohydrazide Release and Antimicrobial Activity

Copolymerization of Quinazolinone Derivatives With Styrene, Methyl Methacrylate and Their Silver Nanocomposites for Biological Applications

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