23,179 results match your criteria ester addition

Interactions of primaquine and chloroquine with PEGylated phosphatidylcholine liposomes.

Sci Rep 2021 Jun 14;11(1):12420. Epub 2021 Jun 14.

Department of Pharmaceutical Sciences, Faculty of Pharmacy, Universitas Airlangga, Nanizar Zaman Joenoes Building, Campus C Unair, Mulyorejo, 60115, Indonesia.

This study aimed to analyze the interaction of primaquine (PQ), chloroquine (CQ), and liposomes to support the design of optimal liposomal delivery for hepatic stage malaria infectious disease. The liposomes were composed of hydrogenated soybean phosphatidylcholine, cholesterol, and distearoyl-sn-glycero-3-phosphoethanolamine-N-(methoxy[polyethyleneglycol]-2000), prepared by thin film method, then evaluated for physicochemical and spectrospic characteristics. The calcein release was further evaluated to determine the effect of drug co-loading on liposomal membrane integrity. Read More

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Acute cardiovascular effects of controlled exposure to dilute Petrodiesel and biodiesel exhaust in healthy volunteers: a crossover study.

Part Fibre Toxicol 2021 Jun 14;18(1):22. Epub 2021 Jun 14.

Department of Public Health and Clinical Medicine, Section of Medicine, Umeå University, Umeå, Sweden.

Background: Air pollution derived from combustion is associated with considerable cardiorespiratory morbidity and mortality in addition to environmental effects. Replacing petrodiesel with biodiesel may have ecological benefits, but impacts on human health remain unquantified. The objective was to compare acute cardiovascular effects of blended and pure biodiesel exhaust exposure against known adverse effects of petrodiesel exhaust (PDE) exposure in human subjects. Read More

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Aldehydes and ketones influence reactivity and selectivity in nickel-catalysed Suzuki-Miyaura reactions.

Chem Sci 2020 Jan 6;11(7):1905-1911. Epub 2020 Jan 6.

WestCHEM Department of Pure and Applied Chemistry, University of Strathclyde 295 Cathedral Street Glasgow G1 1XL Scotland UK

The energetically-favorable coordination of aldehydes and ketones - but not esters or amides - to Ni during Suzuki-Miyaura reactions can lead either to exquisite selectivity and enhanced reactivity, or to inhibition of the reaction. Aryl halides where the C-X bond is connected to the same π-system as an aldehyde or ketone undergo unexpectedly rapid oxidative addition to [Ni(COD)(dppf)] (), and are selectively cross-coupled during competition reactions. When aldehydes and ketones are present in the form of exogenous additives, the cross-coupling reaction is inhibited to an extent that depends on the strength of the coordination of the pendant carbonyl group to Ni. Read More

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January 2020

Copper-catalysed photoinduced decarboxylative alkynylation: a combined experimental and computational study.

Chem Sci 2020 Apr 29;11(19):4939-4947. Epub 2020 Apr 29.

State Key Laboratory of Coordination Chemistry, Jiangsu Key Laboratory of Advanced Organic Materials, School of Chemistry and Chemical Engineering, Nanjing University Nanjing 210023 China

Redox-active esters (RAEs) as alkyl radical precursors have demonstrated great advantages for C-C bond formation. A decarboxylative cross-coupling method is described to afford substituted alkynes from various carboxylic acids using copper catalysts CuCl and Cu(acac). The photoexcitation of copper acetylides with electron-rich NEt as a ligand provides a general strategy to generate a range of alkyl radicals from RAEs of carboxylic acids, which can be readily coupled with a variety of aromatic alkynes. Read More

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Tandem sequential catalytic enantioselective synthesis of highly-functionalised tetrahydroindolizine derivatives.

Chem Sci 2020 Mar 12;11(15):3885-3892. Epub 2020 Mar 12.

EaStCHEM, School of Chemistry, University of St Andrews North Haugh St Andrews KY16 9ST UK

An isothiourea-catalysed enantioselective synthesis of novel tetrahydroindolizine derivatives is reported through a one-pot tandem sequential process. The application of 2-(pyrrol-1-yl)acetic acid in combination with either a trifluoromethyl enone or an α-keto-β,γ-unsaturated ester in an enantioselective Michael addition-lactonisation process, followed by ring-opening and cyclisation, led to a range of 24 tetrahydroindolizine derivatives containing three stereocentres in up to >95 : 5 dr and >99 : 1 er. Read More

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Diastereoselective synthesis of chiral 3-substituted isoindolinones rhodium(III)-catalyzed oxidative C-H olefination/annulation.

Org Biomol Chem 2021 Jun 14. Epub 2021 Jun 14.

College of Chemistry, Green Catalysis Center, Zhengzhou University, Zhengzhou 450001, People's Republic of China.

A new method for the direct and stereoselective synthesis of 3-substituted isoindolinones via Rh(iii)-catalyzed chiral N-sulfinyl amide directed asymmetric [4 + 1] annulation of benzamides with acrylic esters has been developed. The reaction proceeded through an oxidative C-H olefination and a subsequent cyclization by intramolecular aza-Michael addition, producing a series of diastereoisomeric chiral isoindolinones (20 examples) in generally good yields with a dr value up to 5.5 : 1. Read More

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Strain-release 2-azaallyl anion addition/borylation of [1.1.1]propellane: synthesis and functionalization of benzylamine bicyclo[1.1.1]pentyl boronates.

Chem Sci 2021 Apr 14;12(20):7066-7072. Epub 2021 Apr 14.

Roy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania 231 South 34th Street Philadelphia PA USA

We report a 3-component reaction between -benzyl ketimines, [1.1.1]propellane, and pinacol boronates to generate benzylamine bicyclo[1. Read More

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Carbonate-promoted C-H carboxylation of electron-rich heteroarenes.

Chem Sci 2020 Oct 5;11(43):11936-11944. Epub 2020 Oct 5.

Department of Chemistry, Stanford University Stanford California 94305 USA

C-H carboxylation is an attractive transformation for both streamlining synthesis and valorizing CO. The high bond strength and very low acidity of most C-H bonds, as well as the low reactivity of CO, present fundamental challenges for this chemistry. Conventional methods for carboxylation of electron-rich heteroarenes require very strong organic bases to effect C-H deprotonation. Read More

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October 2020

Regioselective addition/annulation of ferrocenyl thioamides with 1,3-diynes a sulfur-transfer rearrangement to construct extended π-conjugated ferrocenes with luminescent properties.

Chem Sci 2020 Sep 16;11(40):11030-11036. Epub 2020 Sep 16.

Key Laboratory of Green Chemistry and Technology of Ministry of Education, College of Chemistry, Sichuan University 29 Wangjiang Road Chengdu 610064 People's Republic of China

Herein a regioselective addition/annulation strategy of ferrocenyl (Fc) thioamides with alkynes to construct thienylferrocene (ThienylFc) structures, involving a rhodium-catalyzed C-H activation, an unusual C2-selective addition of 1,3-diyne, and an unexpected intramolecular sulfur-transfer rearrangement process is described. In this protocol, thioamide not only serves as a directing group to activate the -C-H bond of the ferrocene, but also as a sulfur source to form the thiophene ring. The resulting carboxylic ester group after sulfur transfer can act as a linkage to construct extended π-conjugated ferrocenes (OCTFc) with luminescent properties. Read More

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September 2020

Diverse ring-opening reactions of rhodium η-azaborete complexes.

Chem Sci 2020 Aug 4;11(34):9134-9140. Epub 2020 Aug 4.

Institute for Inorganic Chemistry and Institute for Sustainable Chemistry & Catalysis with Boron, Julius-Maximilians-Universität Würzburg Am Hubland 97074 Würzburg Germany

Sequential treatment of [Rh(COE)Cl] (COE = cyclooctene) with PPr, alkyne derivatives and BuN[triple bond, length as m-dash]BMes (Mes = 2,4,6-trimethylphenyl) provided functionalized rhodium η-1,2-azaborete complexes of the form (η-azaborete)RhCl(PPr). The scope of this reaction was expanded to encompass alkynes with hydrogen, alkyl, aryl, ferrocenyl, alkynyl, azaborinyl and boronate ester substituents. Treatment of these complexes with PMe led to insertion of the rhodium atom into the B-C bond of the BNC ring, forming 1-rhoda-3,2-azaboroles. Read More

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Covalent Adaptable Networks Using β-Amino Esters as Thermally Reversible Building Blocks.

J Am Chem Soc 2021 Jun 14. Epub 2021 Jun 14.

Polymer Chemistry Research Group, Center of Macromolecular Chemistry (CMaC), Department of Organic and Macromolecular Chemistry, Faculty of Science, Ghent University, Krijgslaan 281 S4-bis, Ghent B-9000, Belgium.

In this study, β-amino esters, prepared by the aza-Michael addition of an amine to an acrylate moiety, are investigated as building blocks for the formation of dynamic covalent networks. While such amino esters are usually considered as thermally nondynamic adducts, the kinetic model studies presented here show that dynamic covalent exchange occurs via both dynamic aza-Michael reaction and catalyst-free transesterification. This knowledge is transferred to create β-amino ester-based covalent adaptable networks (CANs) with coexisting dissociative and associative covalent dynamic exchange reactions. Read More

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A pH/HO dual triggered nanoplatform for enhanced photodynamic antibacterial efficiency.

J Mater Chem B 2021 Jun 13. Epub 2021 Jun 13.

School of Materials Science and Engineering, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, China.

Bacterial infection and biofilms cause non-healing chronic wounds and threaten human health. Although antibiotics still play an irreplaceable role to treat infectious diseases in clinics, increasing attention has been paid to the problem of multidrug resistance (MDR). As a novel strategy to deal with bacterial infection, photodynamic antimicrobial therapy (PDAT) has shown promising potential to reduce bacterial infection, and stimuli-responsive nanomaterials have been shown to enhance the antibacterial efficiency and postpone the emergence of drug-resistant bacteria. Read More

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Co-hydrothermal carbonization of swine manure and cellulose: Influence of mutual interaction of intermediates on properties of the products.

Sci Total Environ 2021 May 29;791:148134. Epub 2021 May 29.

School of Material Science and Engineering, University of Jinan, Jinan 250022, China. Electronic address:

Co-hydrothermal carbonization (HTC) of livestock manure and biomass might improve the fuel properties of the hydrochar due to the high reactivity of the biomass-derived intermediates with the abundant oxygen-containing functionalities. However, the complicated compositions make it difficult to explicit the specific roles of the individual components of biomass played in the co-HTC process. In this study, cellulose was used for co-HTC with swine manure to investigate the influence on the properties of the hydrochar. Read More

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Effect of emulsifiers on the discoloration of chlorophyll and their potential for use in green beverages.

J Food Sci 2021 Jun 12. Epub 2021 Jun 12.

Department of Chemistry and Applied Chemistry, Graduate School of Science and Engineering, Saga University, Honjo-machi, Saga, Japan.

The discoloration of chlorophyll (Chl) by light is an ongoing issue for green beverages in the food industry. To suppress the discoloration of Chl in aqueous solution, the effects of different emulsifiers were investigated on the discoloration of Chl under ultraviolet (UV) irradiation to determine their potential application for use as food additives. Sucrose fatty acid ester (SE), sorbitan fatty acid ester (TW), and quillaja saponin (QS) were used as emulsifiers, while Triton X-100 (TX) was used for reference. Read More

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Binding activity of Valeriana fauriei root extract on GABA receptor flunitrazepam sites and distribution of its active ingredients in the brain of mice - a comparison with that of V. officinalis root.

J Ethnopharmacol 2021 Jun 8:114262. Epub 2021 Jun 8.

Department of Pharmacognosy, Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-Dori, Mizuho-ku, Nagoya, Aichi, 467-8603, Japan. Electronic address:

Ethnopharmacological Relevance: Valeriana fauriei root (VF) is a crude drug registered in the Japanese Pharmacopeia 17 Edition and a known substitute for V. officinalis (VO). Although VO has been pharmacologically evaluated for its sedative effects and mechanism of action, data regarding VF remain scarce. Read More

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A reverse catalytic triad Asp containing loop shaping a wide substrate binding pocket of a feruloyl esterase from Lactobacillus plantarum.

Int J Biol Macromol 2021 Jun 9;184:92-100. Epub 2021 Jun 9.

Laboratory of Biomanufacturing and Food Engineering, Institute of Food Science and Technology, Chinese Academy of Agricultural Sciences, Beijing 100193, China. Electronic address:

Feruloyl esterase is an indispensable biocatalyst in food processing, pesticide and pharmaceutical industries, catalyzing the cleavage of the ester bond cross-linked between the polysaccharide side chain of hemicellulose and ferulic acid in plant cell walls. LP_0796 from Lactobacillus plantarum was identified as a feruloyl esterase that may have potential applications in the food industry, but the lack of the substrate recognition and catalytic mechanisms limits its application. Here, LP_0796 showed the highest activity towards methyl caffeate at pH 6. Read More

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Therapeutic Potential of Cannabidiol, Cannabidiolic Acid, and Cannabidiolic Acid Methyl Ester as Treatments for Nausea and Vomiting.

Cannabis Cannabinoid Res 2021 Jun 11. Epub 2021 Jun 11.

Collaborative Neuroscience Program, Department of Psychology, University of Guelph, Guelph, Ontario, Canada.

Nausea and vomiting are the most distressing symptoms reported by oncology patients undergoing anticancer treatment. With the currently available treatments, vomiting and especially nausea remain problematic, highlighting the need for alternative treatments. Here we review and evidence for the effectiveness of the nonpsychoactive cannabinoid cannabidiol (CBD) in managing nausea and vomiting. Read More

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Enantioselective α-Arylation of Primary Alcohols under Sequential One-Pot Catalysis.

J Org Chem 2021 Jun 11. Epub 2021 Jun 11.

University of Strasbourg, CNRS, ISIS UMR 7006, 8 allée Gaspard Monge, 67000 Strasbourg, France.

Secondary benzylic alcohols and diarylmethanols are common structural motifs of biologically active and medicinally relevant compounds. Here we report their enantioselective synthesis by α-arylation of primary aliphatic and benzylic alcohols under sequential catalysis integrating a Ru-catalyzed hydrogen transfer oxidation and a Ru-catalyzed nucleophilic addition. The method can be applied to various alcohols and aryl nucleophiles tolerating a range of functional groups, including secondary alcohols, ketones, alkenes, esters, NH amides, tertiary amines, aryl halides, and heterocycles. Read More

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Humins with Efficient Electromagnetic Wave Absorption: a By-Product of Furfural Conversion  to Isopropyl Levulinate via a Tandem Catalytic Reaction in One-Pot.

Chemistry 2021 Jun 10. Epub 2021 Jun 10.

Jilin University, College of Chemistry, CHINA.

Both one-pot catalytic conversion of furfural (FAL) to isopropyl levulinate (PL) and carbonization of by-product (humins) for electromagnetic wave absorption are discussed, which provides inspiration that humins can be applied to electromagnetic wave absorption. In the former, phosphotungstic acid (PW) is employed as a homogeneous catalyst to convert FAL to PL via a tandem reaction in one pot, with the formation of a vast amount of humins. With FAL and various intermediates as substrates, it was found that humins was a polymerization product of FAL, furfuryl alcohol (FOL) and furfuryl ester (FE) with furan rings. Read More

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Dynamics in Catalytic Asymmetric Diastereoconvergent (3 + 2) Cycloadditions with Isomerizable Nitrones and α-Keto Ester Enolates.

J Am Chem Soc 2021 Jun 9. Epub 2021 Jun 9.

Synthetic Organic Chemistry Laboratory, RIKEN Cluster for Pioneering Research, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan.

Reaction design in asymmetric catalysis has traditionally been predicated on a structurally robust scaffold in both substrates and catalysts, to reduce the number of possible diastereomeric transition states. Herein, we present the stereochemical dynamics in the Ni(II)-catalyzed diastereoconvergent (3 + 2) cycloadditions of isomerizable nitrile-conjugated nitrones with α-keto ester enolates. Even in the presence of multiple equilibrating species, the catalytic protocol displays a wide substrate scope to access a range of CN-containing building blocks bearing adjacent stereocenters with high enantio- and diastereoselectivities. Read More

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Reaching Treatment Goals in Psoriasis with Conventional Systemic Drugs: How Long Are We Willing to Wait?

Dermatology 2021 Jun 9:1-9. Epub 2021 Jun 9.

Psoriasis Center at the Department of Dermatology, University Medical Center Schleswig-Holstein, Kiel, Germany.

Objectives: The purpose of this study was to investigate the attainment of treatment goals according to the European Consensus Programme (ECP-TGs) from 2011 in patients with moderate to severe psoriasis (Pso) treated with the first conventional systemic therapy and to identify factors that might compromise the attainment of these treatment goals.

Methods: In a multicenter, prospective observational study, patients with moderate to severe Pso, defined as either body surface area (BSA) >10% or psoriasis area severity index (PASI) >10 and dermatology life quality index (DLQI) >10, received a conventional systemic therapy that could be modified at each follow-up visit over the course of 18 months. All subjects signed an informed consent form, were ≥18 years of age as well as systemic therapy naïve, and had regular study visits at months 3, 6, 9, 12, and 18 after baseline. Read More

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γ-secretase inhibitors, DAPT and RO4929097, promote the migration of Human Glioma Cells via Smad5-downregulated E-cadherin Expression.

Int J Med Sci 2021 26;18(12):2551-2560. Epub 2021 Apr 26.

Department of Neurosurgery, Chang Gung Memorial Hospital, Chiayi, Taiwan.

Malignant gliomas are a type of central nervous system cancer with extremely high mortality rates in humans. γ-secretase has been becoming a potential target for cancer therapy, including glioma, because of the involvement of its enzymatic activity in regulating the proliferation and metastasis of cancer cells. In this study, we attempted to determine whether γ-secretase activity regulates E-cadherin to affect glioma cell migration. Read More

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The Potential of as a Pigment-Stabilizer to Improve the Pigments Preservation, Flavor Profiles, and Sensory Characteristic of Huangjiu.

Front Microbiol 2021 20;12:678903. Epub 2021 May 20.

Shanghai Engineering Research Center of Food Microbiology, School of Medical Instrument and Food Engineering, University of Shanghai for Science and Technology, Shanghai, China.

Hong Qu Huangjiu (HQW) is distinguished by its inclusion of pigments, meaning that photosensitivity strongly affects the sensory quality of the wine. In this study, the effects of () on the stability of pigments, the flavor profiles, and the sensory characteristics of HQW were investigated. After sterilization, the addition of increased the preservation rate of pigments in HQW by up to 93. Read More

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Plasma lipidome is dysregulated in Alzheimer's disease and is associated with disease risk genes.

Transl Psychiatry 2021 Jun 7;11(1):344. Epub 2021 Jun 7.

Centre for Healthy Brain Ageing (CHeBA), School of Psychiatry, University of New South Wales, Sydney, Australia.

Lipidomics research could provide insights of pathobiological mechanisms in Alzheimer's disease. This study explores a battery of plasma lipids that can differentiate Alzheimer's disease (AD) patients from healthy controls and determines whether lipid profiles correlate with genetic risk for AD. AD plasma samples were collected from the Sydney Memory and Ageing Study (MAS) Sydney, Australia (aged range 75-97 years; 51. Read More

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Opposing responses of the rat pulmonary artery and vein to phenylephrine and other agents in vitro.

BMC Pulm Med 2021 Jun 5;21(1):189. Epub 2021 Jun 5.

Department of Anaesthesia, Obstetrics and Gynecology Hospital, Fudan University, 128 Shenyang road, Shanghai, 200090, China.

Background: Different from current cognition, our study demonstrated that adrenergic receptors agonist phenylephrine significantly relaxed isolated pulmonary artery but constricted pulmonary veins. Through comparing differences in the effects of commonly used vasoactive drugs on pulmonary artery and veins, the study aimed to improve efficiency and accuracy of isolated pulmonary vascular experiments, and to provide experimental basis for clinical drug use.

Methods: The contractile responses of pulmonary arteries and veins from twelve-week-old Male Sprague-Dawley rats to phenylephrine, arginine vasopressin (AVP), U46619, endothelin-1, and potassium chloride (KCl) were recorded, as well as the relaxation in response to phenylephrine, AVP, acetylcholine. Read More

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An integrated overview of bacterial carboxylesterase: Structure, function and biocatalytic applications.

Colloids Surf B Biointerfaces 2021 May 27;205:111882. Epub 2021 May 27.

Enzyme and Microbial Technology Research Centre, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia; Department of Biochemistry, Faculty of Biotechnology and Biomolecular Sciences, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia. Electronic address:

Carboxylesterases (CEs) are members of prominent esterase, and as their name imply, they catalyze the cleavage of ester linkages. By far, a considerable number of novel CEs have been identified to investigate their exquisite physiological and biochemical properties. They are abundant enzymes in nature, widely distributed in relatively broad temperature range and in various sources; both macroorganisms and microorganisms. Read More

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Preparation and properties of poly(L-lactic acid) blends with excellent low-temperature toughness by blending acrylic ester based impact resistance agent.

Int J Biol Macromol 2021 Jun 1;183:1871-1880. Epub 2021 Jun 1.

School of Materials Science and Engineering, Changchun University of Technology, Changchun 130012, China.

Poly(L-lactic acid) (PLLA) blends with excellent low-temperature toughness and strength were prepared by melt compounding with acrylic ester based impact resistance agent (AEIR). The morphology, thermal properties, mechanical properties and biodegradability of the blends were investigated. Morphology observations revealed the blend was immiscible but had good compatibility with the dispersed phase size of about 200-300 nm. Read More

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Prenatal phthalate exposure reduction through an integrated intervention strategy.

Environ Sci Pollut Res Int 2021 Jun 4. Epub 2021 Jun 4.

School of Laboratory Medicine, Hubei University of Chinese Medicine, 16 Huangjia Lake West Road, Wuhan, 430065, China.

Pregnancy represents a sensitive susceptibility window to phthalate esters (PAEs). In this study, we develop an intervention strategy for reducing the exposure of pregnant women to phthalates. Thirty-five pregnant women, who initially underwent maternity examination, were recruited from an ongoing longitudinal prospective prenatal cohort study. Read More

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Multistructural Variational Reaction Kinetics of the Simplest Unsaturated Methyl Ester: H-Abstraction from Methyl Acrylate by H, OH, CH, and HO Radicals.

J Phys Chem A 2021 Jun 3;125(23):5103-5116. Epub 2021 Jun 3.

Key Laboratory of Advanced Technologies of Materials, Ministry of Education, Southwest Jiaotong University, Chengdu, Sichuan 610031, China.

The H-abstraction reaction kinetics of methyl acrylate (MA) + H/OH/CH/HO radicals have been investigated theoretically in the present work. For these reactions, the reaction energies and barrier heights are first computed using several density functionals and compared to the coupled cluster CCSD(T)-F12/jun-cc-pVTZ benchmark calculations. The M062X/maug-cc-pVTZ method shows the best performance with the smallest mean unsigned deviation (MUD) of 0. Read More

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First insight on in vitro metabolism of three newly identified aryl organophosphate esters via a suspect coupled with nontarget screening approach.

Toxicol Lett 2021 May 31;348:73-84. Epub 2021 May 31.

Jiangsu Key Laboratory of Chemical Pollution Control and Resources Reuse, School of Environmental and Biological Engineering, Nanjing University of Science and Technology, Nanjing, 210094, PR China. Electronic address:

The ubiquity of organophosphate esters (OPEs) in the environment has triggered research into metabolic pathways of OPEs. Using liquid chromatography coupled with a hybrid quadrupole Orbitrap high-resolution mass spectrometer, a suspect and characteristic fragment ion-based nontarget screening strategy for the identification of unknown OPE metabolites was developed and evaluated. Then, this integrated approach was successfully used for investigation of three newly identified organophosphate esters (NOPEs), namely 2-biphenylol diphenyl phosphate (BPDPP), tris(2-biphenyl) phosphate (TBPHP), and naphthalen-2-yl diphenyl phosphate (NDPHP), in human liver microsomes (HLMs). Read More

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