Monica Nardi - Academia.edu (original) (raw)
Papers by Monica Nardi
ChemInform, Dec 15, 2011
The presence of Er(OTf)3 allows the synthesis of various heterocyclic ring systems.
ChemInform, Mar 17, 2011
ABSTRACT An eco-compatible method, which permits the formation or cleavage of tert-butyl ethers o... more ABSTRACT An eco-compatible method, which permits the formation or cleavage of tert-butyl ethers of alcohols and phenols, is proposed. The protection step is performed in solvent-free conditions at room temperature using catalytic amount of Er(OTf)(3). The catalyst is easily recovered from the aqueous phase and reused several times without significant loss of activity. The deprotection step developed is also highly eco-friendly since the tert-butyl group is removed very quickly from alcohols and phenols in methanol using MW irradiation.
![Research paper thumbnail of ChemInform Abstract: One-Pot Synthesis of Dibenzo[b,e][1,4]diazepin-1-ones](https://attachments.academia-assets.com/112142732/thumbnails/1.jpg)
](ChemInform, May 31, 2012
A One-Pot Synthesis of Dibenzofurans from 6-Diazo-2-cyclohexenones.-The novel rapid approach is b... more A One-Pot Synthesis of Dibenzofurans from 6-Diazo-2-cyclohexenones.-The novel rapid approach is based on a one-pot Pd-catalyzed cross-coupling/aromatization/Ullmann coupling reaction sequence of 6-diazo-2-cyclohexenones with 2-haloiodobenzenes. The reaction has a broad substrate scope, but does not tolerate 2-bromoiodobenzenes containing electron-withdrawing groups.-(ZHAO, H.; YANG, K.;
ChemInform, Oct 28, 2003
Cerium(III) triflate is a powerful catalyst for the acetylation of alcohols. The reaction works w... more Cerium(III) triflate is a powerful catalyst for the acetylation of alcohols. The reaction works well for a large variety of simple and functionalized alcohols, without isomerisation of chiral centres. Changes of hydroxyl protective groups are possible in a one-pot procedure. The catalyst can be easily recycled.
Scientific Reports, Dec 11, 2019
Green Chemistry
Protection of amine groups by amide formation is still among the preferred strategies for multifu... more Protection of amine groups by amide formation is still among the preferred strategies for multifunctional molecular synthesis despite its waste production, especially the enormous quantities of organic solvents used.
Catalysts
Benzimidazoles and their derivatives play an extraordinarily significant role as therapeutic agen... more Benzimidazoles and their derivatives play an extraordinarily significant role as therapeutic agents, e.g., antiulcer, analgesic, and anthelmintic drugs. The organic synthesis of benzimidazoles and derivatives to obtain active pharmacological compounds represents an important research area in organic chemistry. The use of non-environmental organic compounds and application high energy synthetic methods, the production of waste, and the application of conventional toxic processes are a problem for the pharmaceutical industry and for these important drugs’ synthesis. The substituted benzimidazoles are summarized in this review to provide insight about their organic synthesis using ecofriendly methods, as well as their pharmacological activities.
International Journal of Pharmaceutics
Molecules
The need to develop alternative methods or to use “green” solvents constitutes an essential strat... more The need to develop alternative methods or to use “green” solvents constitutes an essential strategy under the emerging field of green chemistry, particularly in the development of new synthetic strategies in the field of pharmaceutic industry. We report an eco-friendly method of synthesis of poly(2-ethyl-2-oxazoline)-palmitoylate (PEtOz-PA) using Er(OTf)3 as Lewis’s acid catalyst in 2-MeTHF. The novel biomolecule derivative was characterized to confirm palmitoyl group substitution and employed for the formulation, characterization, and antioxidant activity evaluation of curcumin-loaded polymeric micelles.
Heterogeneous bifuctional catalysts are multifunctional synthetic catalysts enabling efficient or... more Heterogeneous bifuctional catalysts are multifunctional synthetic catalysts enabling efficient organic transformations by exploiting two opposite functionalities without mutual destruction. In this paper we report the first Er(III)-based metallorganic heterogeneous catalyst, synthesized by post-calcination MW-assisted grafting and modification of the natural aminoacid L-cysteine. The natural acid-base distance between sites was maintained to assure the cooperation. The applicability of this new bifunctional heterogeneous catalyst to CC bond formation and the supposed mechanisms of action are discussed as well.
1-Indanones have been successfully prepared by means of three different non-conventional techniqu... more 1-Indanones have been successfully prepared by means of three different non-conventional techniques, namely microwaves, high-intensity ultrasound and a Q-tube™ reactor. A library of differently substituted 1-indanones has been prepared via one-pot intramolecular Friedel-Crafts acylation and their efficiency and "greenness" have been compared.
Frontiers in Bioengineering and Biotechnology, 2020
Natural products and herbal therapies represent a thriving field of research, but methods for the... more Natural products and herbal therapies represent a thriving field of research, but methods for the production of plant-derived compounds with a significative biological activity by synthetic methods are required. Conventional commercial production by chemical synthesis or solvent extraction is not yet sustainable and economical because toxic solvents are used, the process involves many steps, and there is generally a low amount of the product produced, which is often mixed with other or similar byproducts. For this reason, alternative, sustainable, greener, and more efficient processes are required. Membrane processes are recognized worldwide as green technologies since they promote waste minimization, material diversity, efficient separation, energy saving, process intensification, and integration. This article describes the production, characterization, and utilization of bioactive compounds derived from renewable waste material (olive leaves) as drug candidates in breast cancer (BC) treatment. In particular, an integrated membrane process [composed by a membrane bioreactor (MBR) and a membrane emulsification (ME) system] was developed to produce a purified non-commercially available phytotherapic compound: the oleuropein aglycone (OLA). This method achieves a 93% conversion of the substrate (oleuropein) and enables the extraction of the compound of interest with 90% efficiency in sustainable conditions. The bioderived compound exercised pro-apoptotic and antiproliferative activities against MDA-MB-231 and Tamoxifen-resistant MCF-7 (MCF-7/TR) cells, suggesting it as a potential agent for the treatment of breast cancer including hormonal resistance therapies.
Electronic Journal of General Medicine, 2018
Introduction: Increasing microbial resistance to antibiotics is one of the main contributors for ... more Introduction: Increasing microbial resistance to antibiotics is one of the main contributors for replacing the appropriate compounds to treat microbial infections. Staphylococcus is one of the most important genera of the bacteria as some strains present on the skin as normal flora and opportunistic infectious agents. Common resistance to antibiotics has been observed in infections caused by this genus from bacteria. Plants have different chemical compounds with antimicrobial properties. The aim of this study was to evaluate the effect of antimicrobial activity of hydroxytyrosol, hydroxytyrosol acetate and hydroxytyrosol oleate which are derived from the leaves of the olive on S. epidermidis and S. aureus. Methods: Hydroxytyrosol, hydroxytyrosol acetate and hydroxytyrosol oleate that are two lipophilic derivatives of hydroxytyrosol, which have been prepared at Magna Graecia University, Italy. The antibiogram test was carried out according to the CLSI guidelines and the Kirby-Bauer method using well assay and Microplate broth dilution for S. aureus and S. epidermidis. Results: The highest Zone of inhibition for the HT, HTA and HTO compounds for Staphylococcus aureus was 30, 19 and 15 mm at a concentration of 100 mg/ml respectively. The highest Zone of inhibition for the HT, HTA and HTO compounds for Staphylococcus epidermidis was 25, 19 and 14 mm at a concentration of 100 mg/ml respectively. The MIC for the above compounds for Staphylococcus aureus was 3.125, 12.5 and 25 mg/ml respectively. The MIC for the above compounds for Staphylococcus epidermidis was 6.25, 12.5 and 50 mg/ml respectively. Conclusion: Respectively, the highest antimicrobial activity against S. aureus and S. epidermidis was evaluated in hydroxytyrosol, hydroxytyrosol acetate and hydroxytyrosol oleate compounds.
Arkivoc, 2006
Erbium triflate is able to afford vic-diacetates in better yields, lower catalyst amounts and sho... more Erbium triflate is able to afford vic-diacetates in better yields, lower catalyst amounts and shorter times than most of the reported methods. Therefore, the present procedure represents a valuable, general and environmentally benign procedure to prepare these compounds.
Foods
The beneficial properties of extra virgin olive oil (EVOO) on lipids blood levels were recognized... more The beneficial properties of extra virgin olive oil (EVOO) on lipids blood levels were recognized by the European Food Safety Authority (EFSA) with a health claim, specifically referring to EVOOs containing at least 5 mg of hydroxytyrosol and its secoiridoids derivatives per 20 g of oil. The main purpose of the work was to characterize the phenolic profile of two commercially available Calabrian monovarietal EVOOs (Nocellara del Belice, VN; Dolce di Rossano, VDR), and to study the effect of one-year storage on secoiridoids composition, by monthly controls. A new UHPLC-ESI-HRMS method was developed and validated, thus facilitating the EFSA claim application and allowing producers to valorize their products. Seven biologically active compounds were chosen: tyrosol, hydroxytyrosol, oleocanthal, oleacein, oleuropein aglycone, verbascoside, and oleuropein. LODs and LOQs were 0.001–0.02 mg g−1 and 0.002–0.08 mg g−1, respectively. The variation coefficients were ≤20% and the percentage of ...
Molecules
Tandem mass spectrometry is proposed to check lipid oxidation, a free radical-mediated phenomenon... more Tandem mass spectrometry is proposed to check lipid oxidation, a free radical-mediated phenomenon which effects oxidative deterioration in polyunsaturated fatty acids. Antioxidants are used by the food industry to delay the oxidation process. This process can be controlled by antioxidants, which may occur as natural constituents of foods or may be intentionally added to products. Synthetic antioxidants such as BHT, BHA, and propyl gallate have been extensively used as antioxidants in the industry. The worldwide tendency to avoid or minimize the use of synthetic food additives has prompted the replacement of synthetic antioxidants with natural analogues. The entire process can be supported by the detection and characterization of the reacting species by suitable application of electrospray tandem mass spectrometry under collision-induced dissociation (ESI-CID-MS/MS). Natural antioxidants were tested in this study to check the oxidative stability of algae oil when adding the natural a...
ChemInform, Dec 15, 2011
The presence of Er(OTf)3 allows the synthesis of various heterocyclic ring systems.
ChemInform, Mar 17, 2011
ABSTRACT An eco-compatible method, which permits the formation or cleavage of tert-butyl ethers o... more ABSTRACT An eco-compatible method, which permits the formation or cleavage of tert-butyl ethers of alcohols and phenols, is proposed. The protection step is performed in solvent-free conditions at room temperature using catalytic amount of Er(OTf)(3). The catalyst is easily recovered from the aqueous phase and reused several times without significant loss of activity. The deprotection step developed is also highly eco-friendly since the tert-butyl group is removed very quickly from alcohols and phenols in methanol using MW irradiation.
ChemInform, May 31, 2012
A One-Pot Synthesis of Dibenzofurans from 6-Diazo-2-cyclohexenones.-The novel rapid approach is b... more A One-Pot Synthesis of Dibenzofurans from 6-Diazo-2-cyclohexenones.-The novel rapid approach is based on a one-pot Pd-catalyzed cross-coupling/aromatization/Ullmann coupling reaction sequence of 6-diazo-2-cyclohexenones with 2-haloiodobenzenes. The reaction has a broad substrate scope, but does not tolerate 2-bromoiodobenzenes containing electron-withdrawing groups.-(ZHAO, H.; YANG, K.;
ChemInform, Oct 28, 2003
Cerium(III) triflate is a powerful catalyst for the acetylation of alcohols. The reaction works w... more Cerium(III) triflate is a powerful catalyst for the acetylation of alcohols. The reaction works well for a large variety of simple and functionalized alcohols, without isomerisation of chiral centres. Changes of hydroxyl protective groups are possible in a one-pot procedure. The catalyst can be easily recycled.
Scientific Reports, Dec 11, 2019
Green Chemistry
Protection of amine groups by amide formation is still among the preferred strategies for multifu... more Protection of amine groups by amide formation is still among the preferred strategies for multifunctional molecular synthesis despite its waste production, especially the enormous quantities of organic solvents used.
Catalysts
Benzimidazoles and their derivatives play an extraordinarily significant role as therapeutic agen... more Benzimidazoles and their derivatives play an extraordinarily significant role as therapeutic agents, e.g., antiulcer, analgesic, and anthelmintic drugs. The organic synthesis of benzimidazoles and derivatives to obtain active pharmacological compounds represents an important research area in organic chemistry. The use of non-environmental organic compounds and application high energy synthetic methods, the production of waste, and the application of conventional toxic processes are a problem for the pharmaceutical industry and for these important drugs’ synthesis. The substituted benzimidazoles are summarized in this review to provide insight about their organic synthesis using ecofriendly methods, as well as their pharmacological activities.
International Journal of Pharmaceutics
Molecules
The need to develop alternative methods or to use “green” solvents constitutes an essential strat... more The need to develop alternative methods or to use “green” solvents constitutes an essential strategy under the emerging field of green chemistry, particularly in the development of new synthetic strategies in the field of pharmaceutic industry. We report an eco-friendly method of synthesis of poly(2-ethyl-2-oxazoline)-palmitoylate (PEtOz-PA) using Er(OTf)3 as Lewis’s acid catalyst in 2-MeTHF. The novel biomolecule derivative was characterized to confirm palmitoyl group substitution and employed for the formulation, characterization, and antioxidant activity evaluation of curcumin-loaded polymeric micelles.
Heterogeneous bifuctional catalysts are multifunctional synthetic catalysts enabling efficient or... more Heterogeneous bifuctional catalysts are multifunctional synthetic catalysts enabling efficient organic transformations by exploiting two opposite functionalities without mutual destruction. In this paper we report the first Er(III)-based metallorganic heterogeneous catalyst, synthesized by post-calcination MW-assisted grafting and modification of the natural aminoacid L-cysteine. The natural acid-base distance between sites was maintained to assure the cooperation. The applicability of this new bifunctional heterogeneous catalyst to CC bond formation and the supposed mechanisms of action are discussed as well.
1-Indanones have been successfully prepared by means of three different non-conventional techniqu... more 1-Indanones have been successfully prepared by means of three different non-conventional techniques, namely microwaves, high-intensity ultrasound and a Q-tube™ reactor. A library of differently substituted 1-indanones has been prepared via one-pot intramolecular Friedel-Crafts acylation and their efficiency and "greenness" have been compared.
Frontiers in Bioengineering and Biotechnology, 2020
Natural products and herbal therapies represent a thriving field of research, but methods for the... more Natural products and herbal therapies represent a thriving field of research, but methods for the production of plant-derived compounds with a significative biological activity by synthetic methods are required. Conventional commercial production by chemical synthesis or solvent extraction is not yet sustainable and economical because toxic solvents are used, the process involves many steps, and there is generally a low amount of the product produced, which is often mixed with other or similar byproducts. For this reason, alternative, sustainable, greener, and more efficient processes are required. Membrane processes are recognized worldwide as green technologies since they promote waste minimization, material diversity, efficient separation, energy saving, process intensification, and integration. This article describes the production, characterization, and utilization of bioactive compounds derived from renewable waste material (olive leaves) as drug candidates in breast cancer (BC) treatment. In particular, an integrated membrane process [composed by a membrane bioreactor (MBR) and a membrane emulsification (ME) system] was developed to produce a purified non-commercially available phytotherapic compound: the oleuropein aglycone (OLA). This method achieves a 93% conversion of the substrate (oleuropein) and enables the extraction of the compound of interest with 90% efficiency in sustainable conditions. The bioderived compound exercised pro-apoptotic and antiproliferative activities against MDA-MB-231 and Tamoxifen-resistant MCF-7 (MCF-7/TR) cells, suggesting it as a potential agent for the treatment of breast cancer including hormonal resistance therapies.
Electronic Journal of General Medicine, 2018
Introduction: Increasing microbial resistance to antibiotics is one of the main contributors for ... more Introduction: Increasing microbial resistance to antibiotics is one of the main contributors for replacing the appropriate compounds to treat microbial infections. Staphylococcus is one of the most important genera of the bacteria as some strains present on the skin as normal flora and opportunistic infectious agents. Common resistance to antibiotics has been observed in infections caused by this genus from bacteria. Plants have different chemical compounds with antimicrobial properties. The aim of this study was to evaluate the effect of antimicrobial activity of hydroxytyrosol, hydroxytyrosol acetate and hydroxytyrosol oleate which are derived from the leaves of the olive on S. epidermidis and S. aureus. Methods: Hydroxytyrosol, hydroxytyrosol acetate and hydroxytyrosol oleate that are two lipophilic derivatives of hydroxytyrosol, which have been prepared at Magna Graecia University, Italy. The antibiogram test was carried out according to the CLSI guidelines and the Kirby-Bauer method using well assay and Microplate broth dilution for S. aureus and S. epidermidis. Results: The highest Zone of inhibition for the HT, HTA and HTO compounds for Staphylococcus aureus was 30, 19 and 15 mm at a concentration of 100 mg/ml respectively. The highest Zone of inhibition for the HT, HTA and HTO compounds for Staphylococcus epidermidis was 25, 19 and 14 mm at a concentration of 100 mg/ml respectively. The MIC for the above compounds for Staphylococcus aureus was 3.125, 12.5 and 25 mg/ml respectively. The MIC for the above compounds for Staphylococcus epidermidis was 6.25, 12.5 and 50 mg/ml respectively. Conclusion: Respectively, the highest antimicrobial activity against S. aureus and S. epidermidis was evaluated in hydroxytyrosol, hydroxytyrosol acetate and hydroxytyrosol oleate compounds.
Arkivoc, 2006
Erbium triflate is able to afford vic-diacetates in better yields, lower catalyst amounts and sho... more Erbium triflate is able to afford vic-diacetates in better yields, lower catalyst amounts and shorter times than most of the reported methods. Therefore, the present procedure represents a valuable, general and environmentally benign procedure to prepare these compounds.
Foods
The beneficial properties of extra virgin olive oil (EVOO) on lipids blood levels were recognized... more The beneficial properties of extra virgin olive oil (EVOO) on lipids blood levels were recognized by the European Food Safety Authority (EFSA) with a health claim, specifically referring to EVOOs containing at least 5 mg of hydroxytyrosol and its secoiridoids derivatives per 20 g of oil. The main purpose of the work was to characterize the phenolic profile of two commercially available Calabrian monovarietal EVOOs (Nocellara del Belice, VN; Dolce di Rossano, VDR), and to study the effect of one-year storage on secoiridoids composition, by monthly controls. A new UHPLC-ESI-HRMS method was developed and validated, thus facilitating the EFSA claim application and allowing producers to valorize their products. Seven biologically active compounds were chosen: tyrosol, hydroxytyrosol, oleocanthal, oleacein, oleuropein aglycone, verbascoside, and oleuropein. LODs and LOQs were 0.001–0.02 mg g−1 and 0.002–0.08 mg g−1, respectively. The variation coefficients were ≤20% and the percentage of ...
Molecules
Tandem mass spectrometry is proposed to check lipid oxidation, a free radical-mediated phenomenon... more Tandem mass spectrometry is proposed to check lipid oxidation, a free radical-mediated phenomenon which effects oxidative deterioration in polyunsaturated fatty acids. Antioxidants are used by the food industry to delay the oxidation process. This process can be controlled by antioxidants, which may occur as natural constituents of foods or may be intentionally added to products. Synthetic antioxidants such as BHT, BHA, and propyl gallate have been extensively used as antioxidants in the industry. The worldwide tendency to avoid or minimize the use of synthetic food additives has prompted the replacement of synthetic antioxidants with natural analogues. The entire process can be supported by the detection and characterization of the reacting species by suitable application of electrospray tandem mass spectrometry under collision-induced dissociation (ESI-CID-MS/MS). Natural antioxidants were tested in this study to check the oxidative stability of algae oil when adding the natural a...