25,980 results match your criteria urea derivatives

Design, synthesis, molecular docking and in silico ADMET profile of pyrano[2,3-d]pyrimidine derivatives as antimicrobial and anticancer agents.

Bioorg Chem 2021 Jul 22;115:105186. Epub 2021 Jul 22.

Department of Biochemistry, Faculty of Science, Ain Shams University, Abbassia, Cairo, Egypt.

Pyrano[2,3-d]pyrimidine derivatives were synthesized by treating cyclic compounds containing active methylene group with aldehyde and malononitrile in butanol. The behavior of pyrano[2,3-d]pyrimidine towards some electrophlies namely triethylorthoformate followed by nitrogen nucleophiles as isobutylamine, urea, phenylthiourea, p-toluidine, o-phenylenediamine, o-aminophenol, 2-amino-4-methyl-pyridine and acetic acid with the aim of obtaining some interesting non-mixed heterocyclic compounds. All synthesized compounds to some extent have shown good antimicrobial activity against different microbial strains that had been extracted by inhibiting cell wall synthesis. Read More

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Synthesis of photoactivable oligosaccharide derivatives from 1,2-cyclic carbamate building blocks and study of their interaction with carbohydrate-binding proteins.

Carbohydr Res 2021 Jul 14;508:108399. Epub 2021 Jul 14.

Institute of Physiology, University of Zurich, Zurich, Switzerland.

Despite the broad occurrence of carbohydrate-protein interactions in biology, the low binding affinities of such interactions hamper the characterization of carbohydrate binding sites in the absence of three-dimensional structural models. To allow the identification of proteins interacting with specific carbohydrate epitopes, we have developed new photoactivable oligosaccharide probes. Oligosaccharides containing the 1,2-cyclic carbamate group were attached to building blocks with a primary amino group to yield the corresponding urea derivatives. Read More

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investigation of nonlinear optical, electronic, and thermodynamic properties of BEDT-TTF molecule: doping with boron.

Heliyon 2021 Jul 3;7(7):e07461. Epub 2021 Jul 3.

Faculty of Science, Department of Physics, University of Yaoundé I, P.M.B 812, Yaoundé, Cameroon.

In this study, the RHF, B3LYP and wB97XD methods with cc-pVDZ basis set have been used to investigate the influence of carbon atoms substitution with boron atoms on the non-linear optical, electronic, optoelectronic and thermodynamic properties of BEDT-TTF ( ). The results show that the undoped molecule denoted BEDT-TTF or ET (Eg = 3.88 eV) and its derivatives are semi-conductors materials. Read More

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Pimavanserin in Dementia-Related Psychosis.

N Engl J Med 2021 07;385(4):372-373

From the Departments of Psychiatry and Neuroscience, Icahn School of Medicine at Mount Sinai, and Delirium Services, Mount Sinai System of Hospitals, New York.

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Trial of Pimavanserin in Dementia-Related Psychosis.

N Engl J Med 2021 07;385(4):309-319

From Banner Alzheimer's Institute and University of Arizona College of Medicine, Phoenix (P.N.T.); Chambers-Grundy Center for Transformative Neuroscience, Department of Brain Health, School of Integrated Health Sciences, University of Nevada, Las Vegas, Las Vegas (J.L.C.); Gérontopôle Alzheimer Clinical and Research Center, Centre Hospitalier Universitaire de Toulouse, Geriatric Department, Maintain Functions and Intrinsic Capacities with Aging Research Team, Center for Epidemiology and Population Health Research, INSERM, Université Paul Sabatier, Toulouse, France (M.E.S.-M.); University of Exeter School of Medicine, Exeter, United Kingdom (C.B.); the Department of Neurology, Oregon Health and Sciences University, Portland (D.E.-L.); the Department of Psychiatry and Human Behavior and the Institute for Memory Impairments and Neurological Disorders, University of California, Irvine, Irvine (D.L.S.), and Acadia Pharmaceuticals, San Diego (B.M., J.M.Y., S.S., E.P.F.) - both in California; the Department of Psychiatry, Columbia University Irving Medical Center, New York (D.P.D.); and Perelman School of Medicine at the University of Pennsylvania, Philadelphia (D.W.).

Background: Patients with dementia due to neurodegenerative disease can have dementia-related psychosis. The effects of the oral 5-HT inverse agonist and antagonist pimavanserin on psychosis related to various causes of dementia are not clear.

Methods: We conducted a phase 3, double-blind, randomized, placebo-controlled discontinuation trial involving patients with psychosis related to Alzheimer's disease, Parkinson's disease dementia, dementia with Lewy bodies, frontotemporal dementia, or vascular dementia. Read More

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Well-Tolerated Amphotericin B Derivatives That Effectively Treat Visceral Leishmaniasis.

ACS Infect Dis 2021 Jul 20. Epub 2021 Jul 20.

Axe des Maladies Infectieuses et Immunitaires du Centre de Recherche du CHU de Québec, Centre de Recherche en Infectiologie, and Département de Microbiologie, Infectiologie et Immunologie, Faculté de Médecine, Université Laval, Québec City, Québec G1V 4G2,Canada.

Chemotherapy against the neglected tropical disease visceral leishmaniasis (VL) is suboptimal with only four licensed drugs. Amphotericin B (AmB), despite its toxicity, remained a second line drug for a long time. However, the demonstration that liposomal AmB is highly effective against VL propelled it, despite its cost, to a first line drug in many countries. Read More

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Organocatalyzed Photoredox Radical Ring-Opening Polymerization of Functionalized Vinylcyclopropanes.

Macromolecules 2020 Oct 1;53(19):8352-8359. Epub 2020 Sep 1.

Department of Chemistry, Colorado State University, Fort Collins, Colorado 80523, United States.

Organocatalyzed photoredox radical ring-opening polymerization (rROP) of vinylcyclopropanes (VCPs) is employed for the synthesis of polymers with controlled molecular weight (MW), dispersity, and composition. Herein, we report the study on the rROP of a variety of VCP monomers bearing diverse functional groups (such as amide, alkene, ketal, urea, hemiaminal ether, and so on) under organocatalyzed conditions with varying light sources and temperature. Notably, VCP monomers bearing natural product functionality or their derivatives can be polymerized in a controlled manner to produce poly(VCPs) with predictable MW, low dispersity, tunable composition, high thermal stability, and tailored glass transition temperature ( ), ranging 39 to 107 °C. Read More

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October 2020

Synthesis and characterization of a series of N, N'-substituted urea derivatives by using electrospray ionization tandem mass spectrometry (ESI-MS/MS): Differentiation of positional isomers.

Rapid Commun Mass Spectrom 2021 Jul 8:e9161. Epub 2021 Jul 8.

Small Molecule Drug Discovery, Bristol Myers Squibb Research and Development, Princeton, New Jersey, United States.

Rationale: Characterization of N,N'-substituted ureas was found to be challenging by NMR, particularly N-di and tri-alkylated ureas because of the absence of adjacent protons. In the present study, electrospray ionization tandem mass spectrometry has been used to differentiate positional isomeric pairs and to characterize a series of N,N'-substituted ureas, as these compounds have significant importance for drug discovery. Additionally, urea is an essential functionality in several bioactive compounds as well as a variety of clinically approved therapies. Read More

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Discovery of memantyl urea derivatives as potent soluble epoxide hydrolase inhibitors against lipopolysaccharide-induced sepsis.

Eur J Med Chem 2021 Jun 29;223:113678. Epub 2021 Jun 29.

Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning, 110016, China. Electronic address:

Sepsis, a systemic inflammatory response, caused by pathogenic factors including microorganisms, has high mortality and limited therapeutic approaches. Herein, a new soluble epoxide hydrolase (sEH) inhibitor series comprising a phenyl ring connected to a memantyl moiety via a urea or amide linkage has been designed. A preferential urea pharmacophore that improved the binding properties of the compounds was identified for those series via biochemical assay in vitro and in vivo studies. Read More

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Design, Synthesis and Anticancer Activity of a New Series of -aryl-'-[4-(pyridin-2-ylmethoxy)benzyl]urea Derivatives.

Molecules 2021 Jun 8;26(12). Epub 2021 Jun 8.

School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China.

The development of cancer treatments requires continuous exploration and improvement, in which the discovery of new drugs for the treatment of cancer is still an important pathway. In this study, based on the molecular hybridization strategy, a new structural framework with an -aryl-'-arylmethylurea scaffold was designed, and 16 new target compounds were synthesized and evaluated for their antiproliferative activities against four different cancer cell lines A549, MCF7, HCT116, PC3, and human liver normal cell line HL7702. The results have shown seven compounds with 1-methylpiperidin-4-yl groups having excellent activities against all four cancer cell lines, and they exhibited scarcely any activities against HL7702. Read More

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PRMT5 Selective Inhibitor Enhances Therapeutic Efficacy of Cisplatin in Lung Cancer Cells.

Int J Mol Sci 2021 Jun 7;22(11). Epub 2021 Jun 7.

College of Medicine, University of Sharjah, Sharjah 27272, United Arab Emirates.

As a therapeutic approach, epigenetic modifiers have the potential to enhance the efficacy of chemotherapeutic agents. Protein arginine methyltransferase 5 (PRMT5), highly expressed in lung adenocarcinoma, was identified to be involved in tumorigenesis. In the current study, we examined the potential antineoplastic activity of PRMT5 inhibitor, arginine methyltransferase inhibitor 1 (AMI-1), and cisplatin on lung adenocarcinoma. Read More

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Design, synthesis and in vitro biological evaluation of a novel class of anti-adenovirus agents based on 3-amino-1,2-propanediol.

Bioorg Chem 2021 Jun 13;114:105095. Epub 2021 Jun 13.

Unit of Infectious Diseases, Microbiology and Preventive Medicine, Institute of Biomedicine of Seville (IBiS), University Hospital Virgen del Rocío/CSIC/University of Seville, E41013 Seville, Spain. Electronic address:

Nowadays there is not an effective drug for the treatment of infections caused by human adenovirus (HAdV) which supposes a clinical challenge, especially for paediatric and immunosuppressed patients. Here, we describe the design, synthesis and biological evaluation as anti-adenovirus agents of a new library (57 compounds) of diester, monoester and triazole derivatives based on 3-amino-1,2-propanediol skeleton. Seven compounds (17, 20, 26, 34, 44, 60 and 66) were selected based on their high anti-HAdV activity at low micromolar concentration (IC from 2. Read More

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Untargeted serum metabolomics and tryptophan metabolism profiling in type 2 diabetic patients with diabetic glomerulopathy.

Ren Fail 2021 Dec;43(1):980-992

Department of Nephrology, the First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan, P.R. China.

Diabetic glomerulopathy (DG) remains the prevalent microvascular complication and leading cause of shortened lifespan in type-2 diabetes mellitus (T2DM) despite improvement in hyperglycemia control. Considering the pivotal role of kidney in metabolism, using untargeted metabolomic techniques to globally delineate the serum metabolite profiles will help advance understanding pathogenetic underpinnings of renal biopsy-confirmed DG from the perspective of metabolism specifically. Fourteen pathologically diagnosed DG patients secondary to T2DM and 14 age- and gender-matched healthy controls (HCs) were recruited for study. Read More

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December 2021

A general procedure for carbon isotope labeling of linear urea derivatives with carbon dioxide.

Chem Commun (Camb) 2021 Jul;57(54):6680-6683

Université Paris Saclay, CEA Service de Chimie Bio-organique et Marquage, DMTS, Gif-sur-Yvette, F-91191, France.

Carbon isotope labeling is a traceless technology, which allows tracking the fate of organic compounds either in the environment or in living organisms. This article reports on a general approach to label urea derivatives with all carbon isotopes, including 14C and 11C, based on a Staudinger aza-Wittig sequence. It provides access to all aliphatic/aromatic urea combinations. Read More

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J Zoo Wildl Med 2021 Jun;52(2):628-637

Zoological Society of London (ZSL), London Zoo, Regent's Park, London, UK, NW1 4RY.

Chronic kidney disease (CKD) is a common cause of morbidity and mortality in captive tigers (). Blood creatinine (Cr) and blood urea nitrogen measurements are inexpensive and common biomarkers used to evaluate renal function. However, several limitations have been reported regarding their sensitivity and interindividual variability. Read More

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Short-term and long-term safety and efficacy of tenofovir alafenamide, tenofovir disoproxil fumarate and entecavir treatment of acute-on-chronic liver failure associated with hepatitis B.

BMC Infect Dis 2021 Jun 14;21(1):567. Epub 2021 Jun 14.

Department of Infectious Diseases, First Affiliated Teaching Hospital, School of Medicine, Xi'an Jiaotong University, Yanta Road (w), No. 277, Xi'an City, 710061, Shaanxi Province, China.

Background & Aims: There is limited evidence on the efficacy and safety of nucleos(t) ide analogues (NAs) in the treatment of HBV-ACLF. Our objective was to evaluate the outcomes among TAF, TDF and ETV, three first-line antivirals against chronic hepatitis B, in patients with HBV-ACLF.

Methods: Patients with HBV-related ACLF were recruited and received daily TAF (25 mg/d), TDF (300 mg/d) and ETV (0. Read More

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Triazine Derivative as Putative Candidate for the Reduction of Hormone-Positive Breast Tumor: , Pharmacological, and Toxicological Approach.

Front Pharmacol 2021 28;12:686614. Epub 2021 May 28.

Department of Pharmacy, COMSAT University, Abbottabad, Pakistan.

Breast cancer is a heterogeneous disease that poses the highest incidence of morbidity among women and presents many treatment challenges. In search of novel breast cancer therapies, several triazine derivatives have been developed for their potential chemotherapeutic activity. This study aims to evaluate the N-nitroso-N-methyl urea (NMU)-induced anti-mammary gland tumor activity of 2,4,6 (O-nitrophenyl amino) 1,3,5-triazine (O-NPAT). Read More

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Inhibitory effect of thiourea derivatives on the growth of blue-green algae.

J Environ Manage 2021 Sep 10;294:113008. Epub 2021 Jun 10.

Faculty of Science and Marine Environment (FSSM), Universiti Malaysia Terengganu, 21030, Kuala Nerus, Terengganu, Malaysia.

High nutrient loading in aquatic environment has become the main causative of harmful algae blooms (HABs) in water resources particularly pond, lake and river. HABs are mostly dominated by microalgae derived from the group of blue-green algae which are capable of releasing harmful toxins. Therefore, this study aims to investigate the inhibitory effects of thiourea derivatives on the growth of such blue-green algae. Read More

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September 2021

Synthesis and antiproliferative screening of novel doubly modified colchicines containing urea, thiourea and guanidine moieties.

Bioorg Med Chem Lett 2021 Jun 8;47:128197. Epub 2021 Jun 8.

Department of Medical Chemistry, Faculty of Chemistry, Adam Mickiewicz University, Uniwersytetu Poznańskiego 8, 61-614 Poznań, Poland. Electronic address:

A new series of 10-demethoxy-10-methylaminocolchicines bearing urea, thiourea or aguanidine moieties at position C7 has been designed, synthesized and evaluated for in vitro anticancer activity against different cancer cell lines (A549, MCF-7, LoVo, LoVo/DX). The majority of the new derivatives were active in the nanomolar range and were characterized by lower IC values than cisplatin or doxorubicin. Two ureas (4 and 8) and thioureas (19 and 25) were found to be good antiproliferative agents (low IC values and high SI) and could prove to be promising candidates for further research in the field of anticancer drugs based on the colchicine skeleton. Read More

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Synthesis of new hydrazone derivatives and evaluation of their monoamine oxidase inhibitory activity.

Bioorg Chem 2021 Jun 1;114:105038. Epub 2021 Jun 1.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Marmara University, Istanbul, Turkey. Electronic address:

A novel series of hydrazone derivatives were designed and synthesized. Their structures were characterized by IR, H NMR, C NMR and HR-MS spectroscopic methods. The newly synthesized compounds were evaluated for their inhibitory activity against monoamine oxidase enzymes (MAO-A and MAO-B). Read More

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Hydrogen-Bonded Dimeric Capsules with Appended Spiropyran Units: Towards Controlled Cargo Release.

Chemistry 2021 Jun 7. Epub 2021 Jun 7.

Institute of Chemical Research of Catalonia (ICIQ), The Barcelona Institute of Science and Technology (BIST), Av. Països Catalans 16, 43007, Tarragona, Spain.

We report the synthesis of unprecedented tetra-urea derivatives of calix[4]arene and calix[4]pyrrole containing four spiropyran (SP) units at their upper rim. We investigate the photo- and acid-induced isomerization of the monomeric and homo-dimeric tetra-ureas derivatives using UV-Vis and H NMR spectroscopies. At micromolar concentration, irradiation of the samples with 365 nm light induces changes in their absorption spectra that are consistent with SP→merocyanine (MC) isomerization. Read More

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The interactions between chiral analytes and chitosan-based chiral stationary phases during enantioseparation.

J Chromatogr A 2021 Aug 18;1650:462259. Epub 2021 May 18.

School of Chemistry and Environmental Engineering, China. Electronic address:

The goal of the present study was to disclose the interactions between chitosan-type chiral selectors (CSs) and chiral analytes during enantioseparation. Hence, six chitosan 3,6-bis(phenylcarbamate)-2-(cyclohexylmethylurea)s were synthesized and characterized. These chitosan derivatives were employed as CSs with which the corresponding coated-type chiral stationary phases (CSPs) were prepared. Read More

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Osmolyte-Induced Effects on the Hydration Behavior and the Osmotic Second Virial Coefficients of Alkyl-Substituted Urea Derivatives: Critical Assessment of Their Structure-Making/Breaking Behavior.

J Phys Chem B 2021 06 4;125(23):6231-6243. Epub 2021 Jun 4.

Department of Chemical Engineering, University of Florida, Gainesville, Florida 32611, United States.

We analyzed the hydration behavior of alkyl-substituted urea osmolytes in terms of their deviation from Lewis-Randall solution ideality and characterized their structure-making/breaking tendency according to a proposed solvation formalism that provides a rigorous cause-effect connection between the system microstructure and its solution thermodynamic nonidealities. After a brief introduction of the rationale behind the use of Lewis-Randall over alternative solution ideality references, we (i) assessed the effect of the nature and type of alkyl substitution on the osmolyte-induced perturbation of the solution microstructure as a function of composition, (ii) analyzed their microstructural responses to changes in temperature and pressure, and (iii) demonstrated the structure-breaking nature of urea and the magnifying behavior of its alkyl-substituted osmolytes, whose trend follows the increasingly positive deviation of the osmolyte solutions from Lewis-Randall ideality. Then, we discussed the falsifiability of a pair of frequently used conjectured structure-making/breaking criteria, supported by the derived exact relationships between the structure-making/breaking parameter, the solution thermodynamic nonideality, and the osmotic second virial coefficient of the aqueous osmolytes. Read More

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Cellulose acetate-polyvinyl alcohol blend hemodialysis membranes integrated with dialysis performance and high biocompatibility.

Mater Sci Eng C Mater Biol Appl 2021 Jul 23;126:112127. Epub 2021 Apr 23.

Department of Bioinformatics and Biotechnology, Government College University, Faisalabad 38000, Pakistan.

Hemodialysis considered as therapy of end-stage renal disease (ESRD) for the separation of protein and uremic toxins based on their molecular weights using semi-permeable membranes. Cellulose Acetate (CA) hemodialysis membrane has been widely used in the biomedical field particularly for hemodialysis applications. The main issue of CA membrane is less selectivity and hemocompatibility. Read More

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Discovery of hydrazide-containing oseltamivir analogues as potent inhibitors of influenza A neuraminidase.

Eur J Med Chem 2021 Oct 23;221:113567. Epub 2021 May 23.

Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang, 110016, PR China. Electronic address:

Neuraminidase (NA) inhibitors play a prime role in treating influenza. However, a variety of viruses containing mutant NAs have developed severe drug resistance towards NA inhibitors, so it is of crucial significance to solve this problem. Encouraged by urea-containing compound 12 disclosed by our lab, we designed a series of oseltamivir derivatives bearing hydrazide fragment for targeting the 150 cavity. Read More

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October 2021

10-Dehydrogingerdione ameliorates renal endoplasmic reticulum/oxidative stress and apoptosis in alcoholic nephropathy induced in experimental rats.

Life Sci 2021 Aug 31;279:119673. Epub 2021 May 31.

Department of Biochemistry, Faculty of Pharmacy, Horus University, Egypt.

Background: Chronic alcoholism induces kidney injury (KI), leading to increased mortality in alcoholic hepatitis patients. Endoplasmic reticulum stress (ER) represents the main initiator of kidney diseases and alcoholic nephropathy.

Aims: We used alcoholic nephropathy rat model followed by 10-dehydrogingerdione (10-DHGD) intake as potential modulator. Read More

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Propellanes as Rigid Scaffolds for the Stereodefined Attachment of σ-Pharmacophoric Structural Elements to Achieve σ Affinity.

Int J Mol Sci 2021 May 26;22(11). Epub 2021 May 26.

Department of Chemistry and Pharamcy, Institut für Pharmazeutische und Medizinische Chemie, Westfälische Wilhelms-Universität Münster, Corrensstraße 48, D-48149 Münster, Germany.

Following the concept of conformationally restriction of ligands to achieve high receptor affinity, we exploited the propellane system as rigid scaffold allowing the stereodefined attachment of various substituents. Three types of ligands were designed, synthesized and pharmacologically evaluated as σ receptor ligands. Propellanes with (1) a 2-methoxy-5-methylphenylcarbamate group at the "left" five-membered ring and various amino groups on the "right" side; (2) benzylamino or analogous amino moieties on the "right" side and various substituents at the left five-membered ring and (3) various urea derivatives at one five-membered ring were investigated. Read More

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Bringing Homogeneous Iron Catalysts on the Heterogeneous Side: Solutions for Immobilization.

Molecules 2021 May 6;26(9). Epub 2021 May 6.

Dipartimento di Chimica Industriale "Toso Montanari", Università degli Studi di Bologna, viale Risorgimento 4, 40136 Bologna, Italy.

Noble metal catalysts currently dominate the landscape of chemical synthesis, but cheaper and less toxic derivatives are recently emerging as more sustainable solutions. Iron is among the possible alternative metals due to its biocompatibility and exceptional versatility. Nowadays, iron catalysts work essentially in homogeneous conditions, while heterogeneous catalysts would be better performing and more desirable systems for a broad industrial application. Read More

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