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Hend A. Alkabes - One of the best experts on this subject based on the ideXlab platform.
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Quinazolinone Derivatives Loaded Polypyrrole/Chitosan Core–Shell Nanoparticles with Different Morphologies: Antibacterial and Anticancer Activities
Nano, 2017Co-Authors: Nehal Salahuddin, Ahmed A. Elbarbary, Hend A. AlkabesAbstract:Polypyrrole/chitosan (PPC) spherical dark nanoparticles surrounded by shadow spheres were fabricated through in situ oxidative polymerization of pyrrole in presence of chitosan (CS) using ferric chloride (FeCl3) as oxidant and evaluated as a carrier for some amino-Quinazolinone derivatives (I–IV). The loading of amino-Quinazolinone derivatives (I–IV) into the core–shell nanoparticles were investigated by thermal gravimetric analysis (TGA). Quinazolinone derivatives (I–IV) loaded nanoparticles showed inter-connected sphere in necklace-like morphology, rods or filaments depending on the functional groups in Quinazolinone derivatives. The release of Quinazolinone derivatives from PPC nanoparticles was pH sensitive. The antimicrobial activity of loaded PPC nanoparticles against gram positive and gram negative bacteria was higher than CS and PPC nanoparticles. The results revealed that new generation of nanoparticles loaded with Quinazolinone represent a potential platform to target breast cancer cell line (MCF7), Ehrlich ascites carcinoma (EAC) cells and liver cancer cells (HEPG2) in comparison with PPC and Quinazolinone derivatives.
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Quinazolinone Derivatives Loaded Polypyrrole/Chitosan Core–Shell Nanoparticles with Different Morphologies: Antibacterial and Anticancer Activities
NANO, 2017Co-Authors: Nehal Salahuddin, Ahmed A. El-barbary, Hend A. AlkabesAbstract:Polypyrrole/chitosan (PPC) spherical dark nanoparticles surrounded by shadow spheres were fabricated through in situ oxidative polymerization of pyrrole in presence of chitosan (CS) using ferric chloride (FeCl3) as oxidant and evaluated as a carrier for some amino-Quinazolinone derivatives (I–IV). The loading of amino-Quinazolinone derivatives (I–IV) into the core–shell nanoparticles were investigated by thermal gravimetric analysis (TGA). Quinazolinone derivatives (I–IV) loaded nanoparticles showed inter-connected sphere in necklace-like morphology, rods or filaments depending on the functional groups in Quinazolinone derivatives. The release of Quinazolinone derivatives from PPC nanoparticles was pH sensitive. The antimicrobial activity of loaded PPC nanoparticles against gram positive and gram negative bacteria was higher than CS and PPC nanoparticles. The results revealed that new generation of nanoparticles loaded with Quinazolinone represent a potential platform to target breast cancer cell line (MC...
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Improvement of antimicrobial activity of Quinazolinone derivatives by loading into chitosan/TPP nanoparticles.
International journal of scientific and research publications, 2016Co-Authors: Nehal Salahuddin, Ahmed A. El-barbary, Hend A. AlkabesAbstract:Chitosan (CS)/Quinazolinone/Tripolyphosphate (TPP) nanoparticles have been synthesized using 2.3:1 molar ratio of CS/TPP in presence of Quinazolinone derivatives (I-IV) through simple one step reaction. The mixture was subjected to ultrasonic waves to obtain the nanoparticles. The nanoparticles are quite uniform in size, spherical shape and rod like structure depending on the Quinazolinone derivatives. The amount of loaded Quinazolinone was calculated using UV-Vis spectrophotometer and TGA. The release of Quinazolinone derivatives (I-IV) in acidic medium (pH=2) is significantly higher than in slightly acidic medium (pH=6.8). The proposed mechanism based on zero orders, first order, Higuchi, Hixson-Crowell and Korsmeyer-Peppas model equation are explored. The antimicrobial activity of nanoparticles was investigated against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus epidermis and Staphylococcus aureas.
Nehal Salahuddin - One of the best experts on this subject based on the ideXlab platform.
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Quinazolinone Derivatives Loaded Polypyrrole/Chitosan Core–Shell Nanoparticles with Different Morphologies: Antibacterial and Anticancer Activities
Nano, 2017Co-Authors: Nehal Salahuddin, Ahmed A. Elbarbary, Hend A. AlkabesAbstract:Polypyrrole/chitosan (PPC) spherical dark nanoparticles surrounded by shadow spheres were fabricated through in situ oxidative polymerization of pyrrole in presence of chitosan (CS) using ferric chloride (FeCl3) as oxidant and evaluated as a carrier for some amino-Quinazolinone derivatives (I–IV). The loading of amino-Quinazolinone derivatives (I–IV) into the core–shell nanoparticles were investigated by thermal gravimetric analysis (TGA). Quinazolinone derivatives (I–IV) loaded nanoparticles showed inter-connected sphere in necklace-like morphology, rods or filaments depending on the functional groups in Quinazolinone derivatives. The release of Quinazolinone derivatives from PPC nanoparticles was pH sensitive. The antimicrobial activity of loaded PPC nanoparticles against gram positive and gram negative bacteria was higher than CS and PPC nanoparticles. The results revealed that new generation of nanoparticles loaded with Quinazolinone represent a potential platform to target breast cancer cell line (MCF7), Ehrlich ascites carcinoma (EAC) cells and liver cancer cells (HEPG2) in comparison with PPC and Quinazolinone derivatives.
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Quinazolinone Derivatives Loaded Polypyrrole/Chitosan Core–Shell Nanoparticles with Different Morphologies: Antibacterial and Anticancer Activities
NANO, 2017Co-Authors: Nehal Salahuddin, Ahmed A. El-barbary, Hend A. AlkabesAbstract:Polypyrrole/chitosan (PPC) spherical dark nanoparticles surrounded by shadow spheres were fabricated through in situ oxidative polymerization of pyrrole in presence of chitosan (CS) using ferric chloride (FeCl3) as oxidant and evaluated as a carrier for some amino-Quinazolinone derivatives (I–IV). The loading of amino-Quinazolinone derivatives (I–IV) into the core–shell nanoparticles were investigated by thermal gravimetric analysis (TGA). Quinazolinone derivatives (I–IV) loaded nanoparticles showed inter-connected sphere in necklace-like morphology, rods or filaments depending on the functional groups in Quinazolinone derivatives. The release of Quinazolinone derivatives from PPC nanoparticles was pH sensitive. The antimicrobial activity of loaded PPC nanoparticles against gram positive and gram negative bacteria was higher than CS and PPC nanoparticles. The results revealed that new generation of nanoparticles loaded with Quinazolinone represent a potential platform to target breast cancer cell line (MC...
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Improvement of antimicrobial activity of Quinazolinone derivatives by loading into chitosan/TPP nanoparticles.
International journal of scientific and research publications, 2016Co-Authors: Nehal Salahuddin, Ahmed A. El-barbary, Hend A. AlkabesAbstract:Chitosan (CS)/Quinazolinone/Tripolyphosphate (TPP) nanoparticles have been synthesized using 2.3:1 molar ratio of CS/TPP in presence of Quinazolinone derivatives (I-IV) through simple one step reaction. The mixture was subjected to ultrasonic waves to obtain the nanoparticles. The nanoparticles are quite uniform in size, spherical shape and rod like structure depending on the Quinazolinone derivatives. The amount of loaded Quinazolinone was calculated using UV-Vis spectrophotometer and TGA. The release of Quinazolinone derivatives (I-IV) in acidic medium (pH=2) is significantly higher than in slightly acidic medium (pH=6.8). The proposed mechanism based on zero orders, first order, Higuchi, Hixson-Crowell and Korsmeyer-Peppas model equation are explored. The antimicrobial activity of nanoparticles was investigated against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus epidermis and Staphylococcus aureas.
Yalin Tang - One of the best experts on this subject based on the ideXlab platform.
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copper catalyzed domino reaction involving c c bond cleavage to construct 2 aryl Quinazolinones
European Journal of Organic Chemistry, 2014Co-Authors: Lixia Wang, Junfeng Xiang, Yalin TangAbstract:A copper-catalyzed approach for the synthesis of 2-aryl-Quinazolinones through a domino reaction involving C–C bond cleavage is described. This protocol involves intramolecular C–C bond cleavage to construct 2-aryl-Quinazolinones, which may offer an alternative method to prepare medically important Quinazolinone derivatives and a new strategy for C–C bond cleavage. Besides C–C bond cleavage, this domino reaction includes N-arylation and benzylic C–H amidation.
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Copper‐Catalyzed Domino Reaction Involving C–C Bond Cleavage To Construct 2‐Aryl Quinazolinones
European Journal of Organic Chemistry, 2014Co-Authors: Li‐xia Wang, Junfeng Xiang, Yalin TangAbstract:A copper-catalyzed approach for the synthesis of 2-aryl-Quinazolinones through a domino reaction involving C–C bond cleavage is described. This protocol involves intramolecular C–C bond cleavage to construct 2-aryl-Quinazolinones, which may offer an alternative method to prepare medically important Quinazolinone derivatives and a new strategy for C–C bond cleavage. Besides C–C bond cleavage, this domino reaction includes N-arylation and benzylic C–H amidation.
Cheng-xue Pan - One of the best experts on this subject based on the ideXlab platform.
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Silver(I)-Catalyzed Selective Hydroalkoxylation of C2-Alkynyl Quinazolinones to Synthesize Quinazolinone-Fused Eight-Membered N,O-Heterocycles
Organic Chemistry Frontiers, 2020Co-Authors: Xiang-fei Kong, Lin-su Wei, Guo Xiuyun, Gu Ziyu, Lu-lu Liu, Cheng-xue PanAbstract:We report a silver-catalyzed hydroalkoxylation of C2-alkynyl Quinazolinones to prepare a series of novel Quinazolinone-fused eight-membered N,O-heterocycles in good-to-excellent yields through a selective 8-endo-dig cyclization. Mechanistic studies revealed that the silver catalyst might aid bidentate coordination of an imine group and alkyne to facilitate 8-endo-dig cyclization to afford eight-membered N,O-heterocycles. Also, the proposed bimetal silver intermediates might promote hydroalkoxylation rapidly for Quinazolinones bearing terminal alkynes at the C2-position. Biological evaluations revealed that most of the designed Quinazolinone-fused eight-membered N,O-heterocycles inhibited nitric-oxide generation significantly in lipopolysaccharide-stimulated RAW264.7 cells and displayed their bioactivity as potentially good anti-inflammatory agents.
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Gold(III)-Catalyzed Selective Cyclization of Alkynyl Quinazolinone-Tethered Pyrroles: Synthesis of Fused Quinazolinone Scaffolds.
The Journal of organic chemistry, 2018Co-Authors: Lin-su Wei, Xiang-fei Kong, Cheng-xue PanAbstract:A series of 1,2- and 2,3-fused Quinazolinones have been synthesized in good to excellent yields through gold-catalyzed selective hydroarylations of alkynyl Quinazolinone-tethered pyrroles. The studies revealed that 1,2-fused Quinazolinones were obtained through a 1,3-rearrangement and sequential 6-exo-trig cyclization of N1-alkynyl Quinazolinone-tethered pyrroles, while N3-alkynyl Quinazolinone-tethered pyrroles went through 6-exo-dig or 7-endo-dig cyclizations directly to afford 2,3-fused Quinazolinones. The fused Quinazolinones could be prepared at gram scale in three steps from commercial ortho-aminobenzamide.
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Gold(III)-Catalyzed Selective Cyclization of Alkynyl Quinazolinone-Tethered Pyrroles: Synthesis of Fused Quinazolinone Scaffolds
2018Co-Authors: Lin-su Wei, Xiang-fei Kong, Cheng-xue PanAbstract:A series of 1,2- and 2,3-fused Quinazolinones have been synthesized in good to excellent yields through gold-catalyzed selective hydroarylations of alkynyl Quinazolinone-tethered pyrroles. The studies revealed that 1,2-fused Quinazolinones were obtained through a 1,3-rearrangement and sequential 6-exo-trig cyclization of N1-alkynyl Quinazolinone-tethered pyrroles, while N3-alkynyl Quinazolinone-tethered pyrroles went through 6-exo-dig or 7-endo-dig cyclizations directly to afford 2,3-fused Quinazolinones. The fused Quinazolinones could be prepared at gram scale in three steps from commercial ortho-aminobenzamide
Umesh A. Kshirsagar - One of the best experts on this subject based on the ideXlab platform.
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Advanced Synthetic Strategies for Constructing Quinazolinone Scaffolds
Synthesis, 2016Co-Authors: Rajendra S. Rohokale, Umesh A. KshirsagarAbstract:Quinazolinones are important heterocyclic scaffolds because of their broad spectrum of medicinal and pharmacological properties. The development of advanced synthetic methods to construct the Quinazolinone motif is therefore an important aspect of synthetic chemistry. This review emphasises the recent developments in methodologies and advanced synthetic strategies for the Quinazolinone core. 1 Introduction 2 Synthesis of 2-Substituted Quinazolinones 2.1 Oxidative Condensation/Cyclization 2.2 Acid-Catalyzed Condensation/Cyclization 2.3 Transition-Metal-Catalyzed C–N Bond Formation 2.4 Transition-Metal-Catalyzed Cyclocarbonylation 3 Synthesis of 3-Substituted Quinazolinones 3.1 Using a Coupling Agent 3.2 Oxidative Condensation/Cyclization 3.3 Transition-Metal-Catalyzed C–N Bond Formation 3.4 Transition-Metal-Catalyzed Cyclocarbonylation 4 Synthesis of 2,3-Disubstituted Quinazolinones 4.1 Dehydrative/Reductive Cyclization 4.2 Oxidative Condensation/Cyclization 4.3 Radical Cyclization 4.4 Transition-Metal-Catalyzed C–N Bond Formation 4.5 Transition-Metal-Catalyzed Cyclocarbonylation 4.6 Acid-Catalyzed Condensation/Cyclization 5 Conclusion
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Recent developments in the chemistry of Quinazolinone alkaloids
Organic & biomolecular chemistry, 2015Co-Authors: Umesh A. KshirsagarAbstract:Quinazolinones, an important class of fused heterocyclic alkaloids has attracted high attention in organic and medicinal chemistry due to their significant and wide range of biological activities. There are approximately 150 naturally occurring Quinazolinone alkaloids known till 2005. Several new Quinazolinone alkaloids (∼55) have been isolated in the last decade. Natural Quinazolinones with exotic structural features and remarkable biological activities have incited a lot of activities in the synthetic community towards the development of new synthetic strategies and approaches for the total synthesis of Quinazolinone alkaloids. This review is focused on these advances in the chemistry of Quinazolinone alkaloids in the last decade. This article covers the newly isolated Quinazolinone natural products with their biological activities and the recently reported total syntheses of Quinazolinone alkaloids from 2006 to 2015.
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hexamethyldisilazane iodine induced intramolecular dehydrative cyclization of diamides a general access to natural and unnatural Quinazolinones
Tetrahedron Letters, 2007Co-Authors: Umesh A. Kshirsagar, Santosh B Mhaske, Narshinha P ArgadeAbstract:Abstract A simple and efficient general approach to various Quinazolinone scaffolds, including peptidomimetic examples, has been demonstrated by employing HMDS/I2 for the intramolecular dehydrative cyclization of diamides. The protecting groups –Boc, –Fmoc and –Cbz tolerated the present reaction conditions and we did not observe any racemization. The present protocol has also been used as a key step for the efficient four-step syntheses of the naturally occurring Quinazolinones, sclerotigenin, (−)-circumdatin-F and (−)-fumiquinazoline-F.
