56,716 results match your criteria range derivatives

Strongly Luminescent Pt(IV) Complexes with a Mesoionic -Heterocyclic Carbene Ligand: Tuning Their Photophysical Properties.

Inorg Chem 2021 May 10. Epub 2021 May 10.

Departamento de Química Inorgánica, Facultad de Química, Universidad de Murcia, Campus de Espinardo 19, 30100 Murcia, Spain.

The synthesis, electrochemistry, and photophysical properties of a series of bis-cyclometalated Pt(IV) complexes that combine the mesoionic aryl-NHC ligand 4-butyl-3-methyl-1-phenyl-1-1,2,3-triazol-5-ylidene (trz) with either 1-phenylpyrazole or 2-arylpyridine (CN) are reported. The complexes (-6-54)-[PtCl(CN)(trz)] bearing cyclometalating 2-arylpyridines present phosphorescent emissions in the blue to yellow color range, which essentially arise from LC(CN) states, and reach quantum yields of ca. 0. Read More

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The revenge of Zygosaccharomyces yeasts in food biotechnology and applied microbiology.

L Solieri

World J Microbiol Biotechnol 2021 May 10;37(6):96. Epub 2021 May 10.

Department of Life Sciences, University of Modena and Reggio Emilia, Via Amendola 2, 42122, Reggio Emilia, Italy.

Non-conventional yeasts refer to a huge and still poorly explored group of species alternative to the well-known model organism Saccharomyces cerevisiae. Among them, Zygosaccharomyces rouxii and the sister species Zygosaccharomyces bailii are infamous for spoiling food and beverages even in presence of several food preservatives. On the other hand, their capability to cope with a wide range of process conditions makes these yeasts very attractive factories (the so-called "ZygoFactories") for bio-converting substrates poorly permissive for the growth of other species. Read More

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ADME properties, bioactivity and molecular docking studies of 4-amino-chalcone derivatives: new analogues for the treatment of Alzheimer, glaucoma and epileptic diseases.

In Silico Pharmacol 2021 3;9(1):34. Epub 2021 May 3.

Department of Chemistry, Faculty of Arts and Sciences, Tokat Gaziosmanpaşa University, 60250 Tokat, Turkey.

In this study, in vitro inhibition effects of (E)-1-(4-aminophenyl)-3-(aryl) prop-2-en-1-one (4-amino-chalcones) derivatives (3a-o) on acetylcholinesterase (AChE) enzyme and human erythrocyte carbonic anhydrase I and II isoenzymes (hCA I- II) were investigated. And also, the biological activities of 4-amino-chalcone derivatives against enzymes which names are acetylcholinesterase (PDB ID: 1OCE), human Carbonic Anhydrase I (PDB ID: 2CAB), human carbonic anhydrase II (PDB ID: 3DC3), were compared. After the results obtained, ADME/T analysis was performed in order to use 4-amino-chalcone derivatives as a drug in the future. Read More

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Fish Oil Improves Pathway-Oriented Profiling of Lipid Mediators for Maintaining Metabolic Homeostasis in Adipose Tissue of Prediabetic Rats.

Front Immunol 2021 21;12:608875. Epub 2021 Apr 21.

Food Science Department, Instituto de Investigaciones Marinas (IIM-CSIC), Vigo, Spain.

Adipose tissue is now recognized as an active organ with an important homeostatic function in glucose and lipid metabolism and the development of insulin resistance. The present research investigates the role of lipid mediators and lipid profiling for controlling inflammation and the metabolic normal function of white adipose tissue from rats suffering from diet-induced prediabetes. Additionally, the contribution to the adipose lipidome induced by the consumption of marine ω-3 PUFAs as potential regulators of inflammation is addressed. Read More

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Design, synthesis and lipid-lowering activities of penipyridone derivatives.

Bioorg Med Chem 2021 May 1;40:116192. Epub 2021 May 1.

Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, People's Republic of China; Laboratory for Marine Drugs and Bioproducts of Qingdao Pilot National Laboratory for Marine Science and Technology, Qingdao 266237, People's Republic of China; Open Studio for Druggability Research of Marine Natural Products, Pilot National Laboratory for Marine Science and Technology, Qingdao 266237, People's Republic of China. Electronic address:

On the basis of our earlier discovered natural product penipyridone G with potential lipid-lowering utility, 35 penipyridone derivatives were designed, synthesized and characterized. Based on the oleic acid-induced HepG2 cell lipid accumulation model, compounds 12c, 14, 15f, 15k, 15o, 15p and 16f showed potent lipid-lowering activities among the synthetic compounds at 10 μM. In particular, compounds 4, 15k, 15o showed significant activities on inhibiting lipid accumulation in insulin resistant HepG2 cells, and these three compounds were safe and non-toxic within the concentration range of 400 μM. Read More

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A study on MAPK/ERK and CDK2-Cyclin-E signal switch "on and off" in cell proliferation by bis urea derivatives of 1, 4-Diisocyanatobenzene.

Bioorg Chem 2021 Apr 23;112:104940. Epub 2021 Apr 23.

Department of Chemistry, Sri Venkateswara Arts College (TTD's), Sri Venkateswara University, Tirupati, Andhra Pradesh, India. Electronic address:

A series of novel substituted bisurea 1,4-Diisocyanatobenzene compounds were designed, synthesized and introduced as potent anticancer compounds and screened for their in vitro anti-proliferative activities in human cancer cell lines. The structures of all titled compounds were characterized using Fourier-transform infrared mass spectra, nuclear magnetic resonance spectroscopy, elemental analysis and evaluated their sustainability using biological experiments. A selected group of ten derivatives were apprised for their anti-proliferative activity. Read More

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Untargeted metabotyping to study phenylpropanoid diversity in crop plants.

Physiol Plant 2021 May 7. Epub 2021 May 7.

Leibniz Institute for Plant Genetics and Crop Plant Research, Gatersleben, Germany.

Plant genebanks constitute a key resource for breeding to ensure crop yield under changing environmental conditions. Because of their roles in a range of stress responses, phenylpropanoids are promising targets. Phenylpropanoids comprise a wide array of metabolites; however, studies regarding their diversity and the underlying genes are still limited for cereals. Read More

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Analysis of boswellic acids in dietary supplements containing Indian frankincense (Boswellia serrata) by Supercritical Fluid Chromatography.

J Pharm Biomed Anal 2021 Apr 27;201:114106. Epub 2021 Apr 27.

Institute of Pharmacy, Pharmacognosy, Center for Molecular Biosciences (CMBI), University of Innsbruck, Innsbruck, Austria. Electronic address:

Boswellic acids, a class of triterpenes, are the bioactive constituents in Indian frankincense, an herbal drug with pronounced anti-inflammatory activity. In this study their separation and quantification in B. serrata extracts is reported for the first time by using Supercritical Fluid Chromatography. Read More

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Concise synthesis and biological evaluation of 2-Aryl-3-Anilinobenzo[b]thiophene derivatives as potent apoptosis-inducing agents.

Bioorg Chem 2021 Apr 20;112:104919. Epub 2021 Apr 20.

Department of Medical Sciences, Laboratory for Technologies of Advanced Therapies (LTTA), University of Ferrara, 44121 Ferrara, Italy.

Many clinically used agents active in cancer chemotherapy exert their activity through the induction of cell death (apoptosis) by targeting microtubules, altering protein function or inhibiting DNA synthesis. The benzo[b]thiophene scaffold holds a pivotal place as a pharmacophore for the development of anticancer agents, and, in addition, this scaffold has many pharmacological activities. We have developed a flexible method for the construction of a new series of 2-aryl-3-(3,4,5-trimethoxyanilino)-6-methoxybenzo[b]thiophenes as potent antiproliferative agents, giving access to a wide range of substitution patterns at the 2-position of the 6-methoxybenzo[b]thiophene common intermediate. Read More

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Determination of tetrabromobisphenol-A/S and their eight derivatives in abiotic (soil/dust) samples using ultra-high performance liquid chromatography-tandem mass spectrometry.

J Chromatogr A 2021 Apr 20;1647:462152. Epub 2021 Apr 20.

State Key Laboratory of Organic Geochemistry, Guangzhou Institute of Geochemistry, Chinese Academy of Sciences, Guangzhou 510640, China; Guangdong-Hong Kong-Macao Joint Laboratory for Environmental Pollution and Control, Guangzhou Institute of Geochemistry, Chinese Academy of Sciences, Guangzhou 510640, People's Republic of China; CAS Center for Excellence in Deep Earth Science, Guangzhou, 510640, China.

Tetrabromobisphenol-A and Tetrabromobisphenol-S (TBBPA/S) and their derivatives have attracted widespread attention owing to their environmental risks and adverse effects on human health. In this study, we developed an analytical method based on ultra-high performance liquid chromatography coupled with triple quadrupole tandem mass spectrometry (UPLC-MS/MS) for the simultaneous determination of TBBPA/S and their eight derivatives in soil samples. After ultrasonic extraction, TBBPA/S and their derivatives were purified using an LC-Si cartridge with 1 mL acetone and 30 mL dichloromethane/n-hexane (1/1, v/v) as the eluent. Read More

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Synthesis and biological evaluation of novel isoxazole-piperazine hybrids as potential anti-cancer agents with inhibitory effect on liver cancer stem cells.

Eur J Med Chem 2021 Apr 24;221:113489. Epub 2021 Apr 24.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, Ankara, Turkey. Electronic address:

In our effort for the development of novel anticancer therapeutics, a series of isoxazole-piperazine analogues were prepared, and primarily screened for their antiproliferative potential against hepatocellular carcinoma (HCC; Huh7/Mahlavu) and breast (MCF-7) cancer cells. All compounds demonstrated potent to moderate cytotoxicity on all cell lines with IC values in the range of 0.09-11. Read More

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Novel inhibitors with sulfamethazine backbone: synthesis and biological study of multi-target cholinesterases and α-glucosidase inhibitors.

J Biomol Struct Dyn 2021 May 5:1-13. Epub 2021 May 5.

Department of Biochemistry, Faculty of Pharmacy, Anadolu University, Eskişehir, Turkey.

The underlying cause of many metabolic diseases is abnormal changes in enzyme activity in metabolism. Inhibition of metabolic enzymes such as cholinesterases (ChEs; acetylcholinesterase, AChE and butyrylcholinesterase, BChE) and α-glucosidase (α-GLY) is one of the accepted approaches in the treatment of Alzheimer's disease (AD) and diabetes mellitus (DM). Here we reported an investigation of a new series of novel ureido-substituted derivatives with sulfamethazine backbone () for the inhibition of AChE, BChE, and α-GLY. Read More

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Visible-Light-Induced Meerwein Fluoroarylation of Styrenes.

Org Lett 2021 May 5. Epub 2021 May 5.

Technical Institute of Fluorochemistry (TIF), Institute of Advanced Synthesis, School of Chemistry and Molecular Engineering, Nanjing Tech University, 30 South Puzhu Road, Nanjing 211816, P. R. China.

An unprecedented approach for assembling a broad range of 1,2-diarylethane derivatives with fluorine-containing fully substituted carbon centers was developed. The protocol features straightforward operation, proceeds under metal-free condition, and accommodates a large variety of synthetically useful functionalities. The critical aspect to the success of this novel transformation lies in using aryldiazonium salts as both aryl radical progenitor and also as single electron acceptor which elegantly enables a radical-polar crossover manifold. Read More

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Stereoselective synthesis of 2-spirocyclopropyl-indolin-3-ones through cyclopropanation of aza-aurones with tosylhydrazones.

Org Biomol Chem 2021 May;19(17):3925-3931

Dipartimento di Scienze Farmaceutiche, Sezione di Chimica Generale e Organica "A. Marchesini", Università degli Studi di Milano, Via G. Venezian 21, 20133, Milano, Italy.

A simple and efficient approach for the synthesis of 2-spirocyclopropyl-indolin-3-ones is herein described. The method involves a diasteroselective cyclopropanation of aza-aurones with tosylhydrazones, selected as versatile carbene sources, and represents a remarkable synthetic alternative to get access to this class of C2-spiropseudoindoxyl scaffolds. The reactions proceed in the presence of a base and catalytic amounts of benzyl triethylammonium chloride and well-tolerate a broad range of substituents on both aza-aurones and tosylhydrazones to afford a series of C2-spirocyclopropanated derivatives in high yields. Read More

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Copper(II)-catalysed direct C3-H esterification of indoles assisted by an ,-bidentate auxiliary moiety.

Org Biomol Chem 2021 May;19(17):3911-3924

College of Pharmaceutical Sciences, Zhejiang University, 866 Yuhangtang Rd., Hangzhou, Zhejiang 310058, China.

The regioselective direct C3-esterification of indoles with OXA is developed in an efficient reaction with carboxylic acids using the catalyst CuBr2 and oxidants Ag2CO3 and K2S2O8. The simple experimental procedure is proved to be broadly applicable to a range of substrates, including aromatic and aliphatic acids, and the corresponding products were obtained in good yields up to 87%. At the same time, it provides a valuable approach to produce C3-benzyl derivatives of indoles through reaction with benzyl carboxylic acid under the same reaction conditions. Read More

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Oral and Topical Vitamin D, Sunshine, and UVB Phototherapy Safely Control Psoriasis in Patients with Normal Pretreatment Serum 25-Hydroxyvitamin D Concentrations: A Literature Review and Discussion of Health Implications.

Nutrients 2021 Apr 29;13(5). Epub 2021 Apr 29.

Wright State University Boonshoft School of Medicine, 3640 Colonel Glenn Hwy, Dayton, OH 45435, USA.

Vitamin D, sunshine and UVB phototherapy were first reported in the early 1900s to control psoriasis, cure rickets and cure tuberculosis (TB). Vitamin D also controlled asthma and rheumatoid arthritis with intakes ranging from 60,000 to 600,000 International Units (IU)/day. In the 1980s, interest in treating psoriasis with vitamin D rekindled. Read More

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2D Honeycomb-Kagome Polymer Tandem as Effective Metal-Free Photocatalysts for Water Splitting.

Adv Mater 2021 May 4:e2008645. Epub 2021 May 4.

TU Dresden Fakultät für Chemie und Lebensmittelchemie, Bergstraße 66c, 01062, Dresden, Germany.

On the basis of first-principles calculations, the potential of applying 2D honeycomb-kagome polymers made of heteroatom-centered triangulene derivatives to photocatalyze water splitting is explored. The designed 2D polymers possess indirect bandgaps in the range of 1.80-2. Read More

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Heterologous Expression of Thermogutta terrifontis Endo-Xanthanase in Penicillium verruculosum, Isolation and Primary Characterization of the Enzyme.

Biochemistry (Mosc) 2021 Apr;86(4):489-495

Federal Research Center "Fundamentals of Fundamental Biotechnology", Russian Academy of Sciences, Moscow, 119071, Russia.

Heterologous endo-xanthanase (EX) from the thermophilic planktomycete Thermogutta terrifontis strain was obtained using Penicillium verruculosum 537 (ΔniaD) expression system with the cellobiohydrolase 1 gene promoter. Homogeneous EX with a molecular weight of 23.7 kDa (pI 6. Read More

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A new flavonoid from the leaves of Craib and α-glucosidase and acetylcholinesterase inhibitory activities.

Nat Prod Res 2021 May 3:1-11. Epub 2021 May 3.

Institute of Chemistry, Vietnam Academy of Science and Technology (VAST), Hanoi, Vietnam.

From the ethyl acetate extract (EtOAc) of the Vietnamese leaves, a new flavone 8--glycoside 2'',6''-di--acetylvitexin (), together with six known analogs were isolated. Their structures were determined by spectral methods and compared with literature data. In α-glucosidase inhibitory assay, the EtOAc extract and its flavone and biflavone derivatives possessed the significant IC range of 9. Read More

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Curcumin, autoimmune and inflammatory diseases: going beyond conventional therapy - a systematic review.

Crit Rev Food Sci Nutr 2020 Dec 1:1-19. Epub 2020 Dec 1.

Medical School of Marília, UNIMAR, Marília, São Paulo, Brazil.

Autoimmune and inflammatory diseases affect innumerous people and are considered a significant cause of morbidity and mortality worldwide and sp can work as important therapies in the approach of these diseases. For this reason the aim of this review is to evaluate the effects of or curcumin in five autoimmune and/or inflammatory diseases for instance, Inflammatory Bowel Disease, Osteoarthritis, Systemic Lupus Erythematous, Psoriasis, and Sclerosis. MEDLINE, EMBASE, and Cochrane Library were searched and PRISMA guidelines were used to build this systematic review. Read More

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December 2020

Determination of nitrofuran metabolites in honey using a new derivatization reagent, magnetic solid-phase extraction and LC-MS/MS.

Talanta 2021 Aug 16;230:122310. Epub 2021 Mar 16.

Central Scientific Methodological Veterinary Laboratory, Orangereynaya st., 23, 111622, Moscow, Russia.

In this study, 5-nitro-2-furaldehyde (5-NFA) was proposed as a new derivatizing agent for nitrofuran metabolites. It reacts with nitrofuran metabolites producing the parent nitrofurans (furazolidone, furaltadone, nitrofurantoin, and nitrofurazone). Magnetic hypercrosslinked polystyrene (HCP/FeO) was first used for magnetic solid phase extraction (MSPE) clean-up before the determination of nitrofuran metabolite derivatives in honey via LC-MS/MS. Read More

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Catalytic fast pyrolysis of waste mixed cloth for the production of value-added chemicals.

Waste Manag 2021 Apr 29;127:141-146. Epub 2021 Apr 29.

Guangzhou Institute of Energy Conversion, Chinese Academy of Sciences (CAS), Guangzhou 510640, PR China; Southern Marine Science and Engineering Guangdong Laboratory (Guangzhou), 511458, PR China; CAS Key Laboratory of Renewable Energy, Guangzhou 510640, PR China; Guangdong Provincial Key Laboratory of New and Renewable Energy Research and Development, Guangzhou 510640, PR China.

In the present study, catalytic fast pyrolysis of waste mixed cloth in an ex-situ method using hierarchical HZSM and commercial CaO was investigated. Pyrolysis of waste mixed cloth in a temperature range of 450 °C to 750 °C mainly allowed for the formation of levoglucosan without any catalysts. The utilization of HZSM with Brønsted/Lewis acid sites on micro- and mesoporous structures significantly contributed to monocyclic/dicyclic chemicals production, mainly referring to monoaromatics and naphthalene-based derivatives, especially in the case of high heating rates and catalyst usages. Read More

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Ocular manifestations of ectodermal dysplasia.

Orphanet J Rare Dis 2021 May 1;16(1):197. Epub 2021 May 1.

Division of Ophthalmology, The Children's Hospital of Philadelphia, 34Th and Civic Center Boulevard, Philadelphia, PA, 19104, USA.

Purpose: The ectodermal dysplasias (EDs) constitute a group of disorders characterized by abnormalities in two or more ectodermal derivatives, including skin, hair, teeth, and sweat glands. The purpose of the current study was to evaluate ocular manifestations in pediatric patients with ED.

Methods: Retrospective case series including consecutive ED subjects who were treated in the ophthalmology department at the Children's Hospital of Philadelphia over a 12-year period (2009-2020). Read More

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An overview of therapeutic potential of N-alkylated 1-deoxynojirimycin congeners.

Carbohydr Res 2021 Apr 16;504:108317. Epub 2021 Apr 16.

School of Chemical Engineering, Nanjing University of Science & Technology, Nanjing, Jiangsu, 210094, PR China. Electronic address:

Polyhydroxylated alkaloids display a wide range of biological activities, suggesting their use in the treatment of various diseases. Their most famous representative, 1-deoxynojirimycin (DNJ), is a natural product that shows α- and β-glucosidase inhibition. This molecule has been since converted into two clinically approved drugs i. Read More

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Design, synthesis and biological evaluation of novel estrone phosphonates as high affinity organic anion-transporting polypeptide 2B1 (OATP2B1) inhibitors.

Bioorg Chem 2021 Apr 20;112:104914. Epub 2021 Apr 20.

Department of Organic Chemistry, University of Szeged, Dóm tér 8, H-6720 Szeged, Hungary. Electronic address:

Organic anion-transporting polypeptide 2B1 (OATP2B1) is a multispecific membrane transporter mediating the cellular uptake of various exo- and endobiotics, including drugs and steroid hormones. Increased uptake of steroid hormones by OATP2B1 may increase tumor proliferation. Therefore, understanding OATP2B1's substrate/inhibitor recognition and inhibition of its function, e. Read More

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Novel 2,5-disubstituted-1,3,4-oxadiazole derivatives as MAO-B inhibitors: Synthesis, biological evaluation and molecular modeling studies.

Bioorg Chem 2021 Apr 16;112:104917. Epub 2021 Apr 16.

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

Thirty novel 2,5-disubstituted-1,3,4-oxadiazole derivatives bearing urea moiety were designed and synthesized. IR, H-NMR, C-NMR and mass spectroscopic methods and elemental analysis were used to confirm the structures of the compounds. Their monoamine oxidase inhibitory activity was determined against the MAO-A and MAO-B isoforms. Read More

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Regioselective synthesis of triazolo[3,4-]purine derivatives and their anti-cancer activity against NCI-60 cell-lines.

Folia Med (Plovdiv) 2021 Apr;63(2):213-220

Saurashtra University, Rajkot, India.

Introduction: Due to the vast medicinal importance of purine nucleoside, a hybrid molecule of triazole with purine ring might explode a lead molecule in the pharma sector and based on the last decade's studies suggested that the nitrogen-rich molecules possess a wide range of medicinal importance.

Aim: Due to the vast application of purine nucleoside itself in the field of cancer research, we synthesized triazolo[3,4-e]purines and screened them for their anti-cancer study against NCI-60 cell lines by the protocol used by NIH.

Materials And Methods: The targeted molecules, 4-chloro-5a,6-dihydro-8-substitutedphenyl-1H-[1,2,4]triazolo[3,4-e]purine derivatives (4a-4h) were synthesized in a two-step procedure by nucleophilic substitution (SN) at C-2 chlorine followed by formation of the triazole ring by acid-catalyzed reaction in the polar protic solvent. Read More

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Screening of Antioxidative Properties and Inhibition of Inflammation-Linked Enzymes by Aqueous and Ethanolic Extracts of Plants Traditionally Used in Wound Healing in Poland.

Antioxidants (Basel) 2021 Apr 28;10(5). Epub 2021 Apr 28.

Department of Pharmacognosy and Molecular Basis of Phytotherapy, Warsaw Medical University, Banacha 1, 02-097 Warsaw, Poland.

A wide range of plant-derived preparations have been used against skin inflammatory disorders and as wound healing agents in traditional medicine. The purpose of the study was to determine the antioxidant activity of aqueous and 70% ethanolic extracts from eleven species of plants traditionally used in Poland to treat inflammatory skin diseases. The ability of extracts to scavenge 2,2-diphenyl-1-picrylhydrazyl radical (DPPH), hydrogen peroxide (HO), and superoxide anion (O), was studied. Read More

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Characterization of Subtype Selective Cannabinoid CB Receptor Agonists as Potential Anti-Inflammatory Agents.

Pharmaceuticals (Basel) 2021 Apr 19;14(4). Epub 2021 Apr 19.

Department of Pharmaceutical Sciences, University of Connecticut, Storrs, CT 06269, USA.

Activation of the CB receptor has been shown to have anti-inflammatory and antinociceptive effects without causing psychoactive effects. Previously, we reported that the compound ethyl 2(2-(-(2,3-dimethylphenyl) phenylsulfonamido)acetamido)benzoate (ABK5) is a CB subtype selective agonist with anti-inflammatory and antinociceptive effects. In the present study, we tested four ABK5 derivatives, ABK5-1, ABK5-2, ABK5-5, and ABK5-6, to analyze the structure of ABK5 to obtain CB-selective agonists with higher affinity and efficacy. Read More

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Synthesis of 4-Arylselanyl-1-1,2,3-triazoles from Selenium-Containing Carbinols.

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

LASOL-CCQFA, Universidade Federal de Pelotas-UFPel, P.O. Box 354, 96010-900 Pelotas, Brazil.

In this work, we present a simple way to achieve 4-arylselanyl-1-1,2,3-triazoles from selenium-containing carbinols in a one-pot strategy. The selenium-containing carbinols were used as starting materials to produce a range of selanyl-triazoles in moderate to good yields, including a quinoline and Zidovudine derivatives. One-pot protocols are crucial to the current concerns about waste production and solvent consumption, avoiding the isolation and purification steps of the reactive terminal selanylalkynes. Read More

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