76,624 results match your criteria compounds amino


Biology-oriented drug synthesis and evaluation of secnidazole esters as novel enzyme ınhibitors.

Arch Pharm (Weinheim) 2021 Dec 3:e2100376. Epub 2021 Dec 3.

Department of Chemistry, Federal Urdu University of Art, Science and Technology, Karachi, Pakistan.

The identification of novel compounds that can inhibit physiologically and metabolically important drug targets or enzymes has prime importance in medicinal chemistry. With this aim, a range of secnidazole esters 1-30 were synthesized under the heading of biology-oriented drug synthesis by the 1,1'-carbonyldiimidazole-mediated coupling reaction between secnidazole and varyingly benzoic acid derivatives. All compounds were screened for inhibitory activity against human carbonic anhydrase (hCA) I and II, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-glucosidase. Read More

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December 2021

Design, synthesis, in vitro antiproliferative evaluation and GSK-3β kinase inhibition of a new series of pyrimidin-4-one based amide conjugates.

Bioorg Chem 2021 Nov 26;119:105512. Epub 2021 Nov 26.

Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110 062, India.

A new series of novel amide conjugates of pyrimidin-4-one and aromatic/heteroaromatic /secondary cyclic amines has been synthesized and their in vitro antiproliferative activities against a panel of 60 human cancer cell lines of nine different cancer types were tested at NCI. Among the synthesized compounds, compound (4i) showed significant anti-proliferative activity. Compound (4i) displayed most potent activity against the breast tumor cell line T-47D and CNS tumor cell line SNB-75 exhibiting a growth of 1. Read More

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November 2021

The GH3 amidosynthetases family and their role in metabolic crosstalk modulation of plant signaling compounds.

Phytochemistry 2021 Nov 30;194:113039. Epub 2021 Nov 30.

Department of Biochemistry, Nicolaus Copernicus University in Torun, Lwowska 1, 87-100, Torun, Poland. Electronic address:

The Gretchen Hagen 3 (GH3) genes encoding proteins belonging to the ANL superfamily are widespread in the plant kingdom. The ANL superfamily consists of three groups of adenylating enzymes: aryl- and acyl-CoA synthetases, firefly luciferase, and amino acid-activating adenylation domains of the nonribosomal peptide synthetases (NRPS). GH3s are cytosolic, acidic amidosynthetases of the firefly luciferase group that conjugate auxins, jasmonates, and benzoate derivatives to a wide group of amino acids. Read More

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November 2021

Nitriles as main products from the oxidation of primary amines by ferrate(VI): Kinetics, mechanisms and toxicological implications for nitrogenous disinfection byproduct control.

Water Res 2021 Nov 19;209:117881. Epub 2021 Nov 19.

School of Earth Sciences and Environmental Engineering, Gwangju Institute of Science and Technology (GIST), Gwangju 61005, Republic of Korea. Electronic address:

Ferrate (Fe(VI)), a promising water treatment oxidant, can be used for micropollutant abatement or disinfection byproduct mitigation. However, knowledge gaps remain concerning the interaction between Fe(VI) and dissolved organic matter structures, notably primary amines. This study investigated degradation kinetics and products of several aliphatic primary amines by Fe(VI). Read More

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November 2021

Ratiometric Fluorescent Sensor for Copper(II) and Phosphate Ions from Aminopyrene Derivatives.

Photochem Photobiol 2021 Dec 3. Epub 2021 Dec 3.

Department of Chemistry, Faculty of Science, Chulalongkorn University, Bangkok, 10330, Thailand.

Three derivatives of 1-aminopyrene are functionalized with 2-picolyl and 2-picolinyl groups and tested as fluorescent sensors for metal ions. The target compounds are successfully synthesized in 50 to 90% yields and characterized by H-NMR, C-NMR, and HRMS. The compound with an amino picolyl group (P1) exhibits an excellent selectivity towards Cu(II) ion as the fluorescent signal shifts from 433 to 630 nm. Read More

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December 2021

Genome and Analysis of the Probiotic Properties of a Bacterial Endophyte, Strain MHSD3.

Front Genet 2021 11;12:672149. Epub 2021 Nov 11.

Department of Biotechnology and Food Technology, University of Johannesburg, Johannesburg, South Africa.

Sporeforming species are gaining interest in human health recently, due to their ability to withstand the harsh environment of the gastrointestinal tract. The present study explores probiotic features of strain MHSD3 through genomic analysis and probiotic assays. The draft genome of strain MHSD3 contained genes associated with tolerance to gastrointestinal stress and adhesion. Read More

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November 2021

Target specificity of selective bioactive compounds in blocking α-dystroglycan receptor to suppress Lassa virus infection: an approach.

J Biomed Res 2021 Nov;35(6):459-473

Department of Electrical and Electronic Engineering, United International University, Dhaka 1212, Bangladesh.

Lassa hemorrhagic fever, caused by Lassa mammarenavirus (LASV) infection, accumulates up to 5000 deaths every year. Currently, there is no vaccine available to combat this disease. In this study, a library of 200 bioactive compounds was virtually screened to study their drug-likeness with the capacity to block the α-dystroglycan (α-DG) receptor and prevent LASV influx. Read More

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November 2021

Synthesis of a covalent organic framework with hydrazine linkages and its application in open-tubular capillary electrochromatography.

J Chromatogr A 2021 Nov 12;1661:462681. Epub 2021 Nov 12.

State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, China; College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, China.

Recently, covalent organic frameworks (COFs), owning to their excellent and unique properties, are attracting the attention of numerous researchers in some areas, especially the domain of chromatographic separation. However, the application of hydrazine linkages COFs in open-tubular capillary electrochromatography (OT-CEC) lies in the early stage at present. Herein, a well-crystallized hydrazine-linked COF (Tf-DHzOH) was synthesized successfully from 2,5-dihydroxyterephtalohydrazide and 1,3,5-triformyl-benzene. Read More

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November 2021

Design, Synthesis, Structural Optimization, SAR, in silico Prediction of Physicochemical Properties and Pharmacological Evaluation of Novel & Potent Thiazolo[4,5-d]pyrimidine Corticotropin Releasing Factor (CRF) Receptor Antagonists.

Eur J Pharm Sci 2021 Nov 29:106084. Epub 2021 Nov 29.

Department of Pharmaceutical Science, College of Pharmacy & Allied Health Professions, South Dakota State University, Brookings, SD, 57007, USA. Electronic address:

Corticotropin-releasing factor (CRF) is a 41-amino-acid neuropeptide secreted from the hypothalamus and is the main regulator of the hypothalamus-pituitary-adrenocortical (HPA) axis. CRF is the master hormone which modulates physiological and behavioral responses to stress. Many disorders including anxiety, depression, addictive disorders and others are related to over activation of the CRF system. Read More

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November 2021

FT-IR and synchronous fluorescence two-dimensional correlation spectroscopic analysis on the binding properties of mercury onto humic acids as influenced by pH modification and sulfide addition.

Sci Total Environ 2021 Nov 29:152047. Epub 2021 Nov 29.

Key Laboratory of Microbial Technology for Industrial Pollution Control of Zhejiang Province, College of Environment, Zhejiang University of Technology, Hangzhou 310014, China. Electronic address:

Mercuric Hg ion forms strong complexes with dissolved organic matter (DOM) in natural waters. The complexation of Hg by sulfhydryl groups of DOM was regarded as the main mechanism for Hg-DOM interactions, particularly in anoxic sulfur and DOM-rich environments. In the present study, the influences of pH and sulfide addition on the molecular structure of Hg-DOM complexes and the characteristics of Hg binding to DOM were investigated using FT-IR and synchronous fluorescence two-dimensional correlation spectroscopic analysis. Read More

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November 2021

A conformationally stable acyclic β-hairpin scaffold tolerating the incorporation of poorly β-sheet-prone amino acids.

Chembiochem 2021 Dec 1. Epub 2021 Dec 1.

University of Salzburg, Research Centre of Biosciences and Health Department of Molecular Biology, Billrothstra�e 11, 5020, Salzburg, AUSTRIA.

The β-hairpin is a structural element of native proteins, but it is also a useful artificial scaffold for finding lead compounds to convert into peptidomimetics or non-peptide structures for drug discovery. Since linear peptides are synthetically more easily accessible than cyclic ones, but are structurally less well-defined, we propose XWXWXpPXK(/R)X(R) as an acyclic but still rigid β-hairpin scaffold that is robust enough to accommodate different types of side chains, regardless of the secondary-structure propensity of the X residues. The high conformational stability of the scaffold results from tight contacts between cross-strand cationic and aromatic side chains, combined with the strong tendency of the d-Pro-l-Pro dipeptide to induce a type II' β-turn. Read More

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December 2021

Synthesis of bitopic ligands as potent dopamine D2 receptor agonists.

ChemMedChem 2021 Dec 2. Epub 2021 Dec 2.

Changzhou University, School of Pharmacy, 1 Gehu Road, Wujin District, 213164, Changzhou, CHINA.

In this study, we designed and synthesized twelve bitopic ligands as dopamine D2 receptor (D2R) agonists. The forskolin-induced cAMP accumulation assay revealed that all the finial compounds are able to activate D2R. Furthermore, compound 11b showed 21-fold higher potency than lead compound 2 and 17-fold higher subtype selectivity for D2R over D4R, indicating that the optimal length of spacer affects the D2R functionality. Read More

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December 2021

In silico and in vivo neuropharmacological evaluation of two γ-amino acid isomers derived from 2,3-disubstituted benzofurans, as ligands of GluN1-GluN2A NMDA receptor.

Amino Acids 2021 Dec 2. Epub 2021 Dec 2.

Instituto de Ciencias Básicas Universidad Veracruzana, Av. Dr. Luis Castelazo Ayala s/n Col. Industrial Animas, Xalapa, 91190, Veracruz, Mexico.

The GABAergic and glutamatergic neurotransmission systems are involved in seizures and other disorders of the central nervous system (CNS). Benzofuran derivatives often serve as the core in drugs used to treat such neurological disorders. The aim of this study was to synthesize new γ-amino acids structurally related to GABA and derived from 2,3-disubstituted benzofurans, analyze in silico their potential toxicity, ADME properties, and affinity for the GluN1-GluN2A NMDA receptor, and evaluate their potential activity and neuronal mechanisms in a murine model of pentylenetetrazol (PTZ)- and 4-aminopyridine (4-AP)-induced seizures. Read More

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December 2021

Amino-Functionalized Cage-Opened C Derivatives.

Org Lett 2021 Dec 2. Epub 2021 Dec 2.

Institute for Chemical Research, Kyoto University, Uji, Kyoto 611-0011, Japan.

The amino-functionalized cage-opened [60]fullerene derivatives were synthesized by reactions with phenylenediamine. In this reaction, the diamine undergoes direct addition to the α,β-unsaturated carbonyl moiety. Further C-C bond scission is promoted by the intramolecular S2 reaction. Read More

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December 2021

Synthesis and evaluation of antioxidant, anti-edematogenic and antinociceptive properties of new selenium-sulfa compounds.

ChemMedChem 2021 Dec 1. Epub 2021 Dec 1.

Universidade Federal de Pelotas, CCQFA, Campus Capão do Leão, 96010900, Pelotas, BRAZIL.

We describe here results for the synthesis and synthetic application of 4-amino-3-(arylselanyl)benzenesulfonamides, and preliminary evaluation of antioxidant, anti-edematogenic and antinociceptive properties. This class of compounds was synthesized in good yields by a reaction of commercially available sulfanilamide and diorganyl diselenides in the presence of 10 mol% of I 2 . Furthermore, the synthesized compound 3a was evaluated on complete Freund's adjuvant (CFA)-induced acute inflammatory pain. Read More

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December 2021

Development of Novel Methodology Using Diazo Compounds and Metal Catalysts.

Authors:
Shingo Harada

Chem Pharm Bull (Tokyo) 2021 ;69(12):1170-1178

Graduate School of Pharmaceutical Sciences, Chiba University.

The ability to control the reactions of highly active chemical species to enable straightforward synthesis of valuable compounds such as bioactive natural products and pharmaceuticals is a continuing challenge in synthetic organic chemistry. This review describes the development of a methodology using reactive metal-carbene species and its synthetic application in our laboratory. First, regioselective synthesis of γ-amino acid equivalents to take advantage of their metal-dependent reactivities and the mechanistic rationale are presented. Read More

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January 2021

Synthesis and in vitro antifungal activity of new Michael-type amino derivatives of xanthatin, a natural sesquiterpene lactone from Xanthium strumarium L.

Bioorg Med Chem Lett 2021 Nov 28;55:128481. Epub 2021 Nov 28.

College of Plant Protection, Shanxi Agricultural University, Taigu 030801, Shanxi Province, PR China. Electronic address:

Structural optimization using plant secondary metabolites as templates is one of the important approach to discover pesticide molecules with novel skeletons. Xanthatin, a natural sesquiterpene lactone isolated from the Xanthium plants (Family: Compositae), exhibits important biological properties. In this work, a series of Michael-type amino derivatives were prepared from xanthatin and their structures were characterized by H NMR, C NMR and HR-MS, and their antifungal activities against several phytopathogenic fungi were evaluated according to the spore germination method and mycelium growth rate method in vitro. Read More

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November 2021

Anti-obesity effect of Auricularia heimuer fruiting body alcohol extraction on obese mice and crucial metabolite pathway analysis by liquid chromatography-tandem mass spectrometry.

J Food Biochem 2021 Dec 1:e14002. Epub 2021 Dec 1.

College of Food Sciences, Fujian Agriculture and Forestry University, Fuzhou, China.

In recent years, the increasing obese and overweight population has become a worldwide public health problem, as there is no effective medication to control obesity. Auricularia heimuer is rich in active substances that have potential biologically active functions. The anti-obesity effect and mechanism of Auricularia heimuer fruiting body alcohol extraction (AHA, 150-600 mg/kg·bw) was investigated in obese mice by assessing changes in endogenous liver metabolites using a liquid chromatography-tandem mass spectrometry approach. Read More

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December 2021

Assessment of the risks of copper- and zinc oxide-based nanoparticles used in Vigna radiata L. culture on food quality, human nutrition and health.

Environ Geochem Health 2021 Dec 1. Epub 2021 Dec 1.

Plant Toxicology and Molecular Biology of Microorganisms, Faculty of Sciences of Bizerta, Zarzouna, Tunisia.

The present article aims to assess the phytotoxic effects of copper and zinc oxide nanoparticles (Cu NPs, ZnO NPs) on mung bean (Vigna radiata L.) and their possible risk on food quality and safety. We also study the molecular mechanisms underlying the toxicity of nanosized Cu and ZnO. Read More

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December 2021

Biochemical Characterization and Storage Stability of Process Waters from Industrial Shrimp Production.

ACS Omega 2021 Nov 10;6(46):30960-30970. Epub 2021 Nov 10.

Food and Nutrition Science, Biology and Biological Engineering, Chalmers University of Technology, Gothenburg 412 96, Sweden.

Shrimp boiling water (SBW) and shrimp peeling water (SPW), generated during shrimp processing, were characterized in terms of crude composition, volatile compounds, as well as nutritional and potentially toxic elements over a 13 month sampling period. The storage stability of both waters was also evaluated. Results showed that SBW contained on median 14. Read More

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November 2021

Application of the dual-tail approach for the design and synthesis of novel Thiopyrimidine-Benzenesulfonamide hybrids as selective carbonic anhydrase inhibitors.

Eur J Med Chem 2021 Nov 20;228:114004. Epub 2021 Nov 20.

Università Degli Studi di Firenze, Department NEUROFARBA - Pharmaceutical and Nutraceutical Section, University of Firenze, Via Ugo Schiff 6, I-50019, Sesto Fiorentino, Firenze, Italy. Electronic address:

A dual-tail approach was applied to the design of a novel series of 2-thiopyrimidine-benzenesulfonamides as carbonic anhydrase (CA) inhibitors. The design strategy is based on the hybridization between a benzenesulfonamide moiety as Zn binding group and 2,4-disubstituted thiopyridimidine as a tail. Among the synthesized compounds, 14h displayed the highest potency (K = 1. Read More

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November 2021

Reactions of amines with ozone and chlorine: Two novel oxidative methods to evaluate the N-DBP formation potential from dissolved organic nitrogen.

Water Res 2021 Nov 13;209:117864. Epub 2021 Nov 13.

School of Architecture, Civil and Environmental Engineering (ENAC), Ecole Polytechnique Fédérale de Lausanne (EPFL), Lausanne 1015, Switzerland; Eawag, Swiss Federal Institute of Aquatic Science and Technology, Überlandstrasse 133, Dübendorf 8600, Switzerland; Institute of Biogeochemistry and Pollutant Dynamics, ETH Zürich, Zürich 8092, Switzerland. Electronic address:

The composition of oxidant-reactive dissolved organic nitrogen (DON) is poorly characterized, although its ozonation is likely to form a great variety of disinfection by-products containing a nitrogen-oxygen bond (N-DBPs). In this study, two chemical oxidation procedures were developed: continuous ozonation at pH 7.0 and free available chlorine (FAC) titrations at pH 9. Read More

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November 2021

Nucleophilic Catalyzed Structural Binary Cleavage of a Fused [5,5]-Bicyclic Compound.

Org Lett 2021 Nov 30. Epub 2021 Nov 30.

Department of Chemistry, University of Idaho, Moscow, Idaho 83844-2343 United States.

Structural binary cleavage of 3,7-diamino-2,6-dinitro-1,5-pyrazolo-[1,2-]pyrazole-1,5-dione , under nucleophilic conditions, leads to the formation of a monocyclic pyrazole unit of 5-amino-4-nitro-1,2-dihydro-3-pyrazol-3-one, . Additionally, various salts of the pyrazole ring were synthesized and fully characterized. Detonation properties and mechanical sensitivities of and other new compounds are remarkably improved compared to . Read More

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November 2021

Integrated computational approach for design of new purinyl pyridine derivatives as B-Raf kinase inhibitors.

J Recept Signal Transduct Res 2021 Nov 29:1-15. Epub 2021 Nov 29.

Department of Chemistry, University College of Science, Osmania University, Hyderabad, India.

B-Raf is one among the most frequently mutating proto-oncogene which is associated with the serine/threonine Raf kinase family involved in the RAS-RAF-MEK-ERK pathway, which is the most deregulated pathway in human cancers. Mutant B-Raf got an excellent scope for investigation in cancer as a potential therapeutic target. Formerly B-Raf is considered the molecular target for numerous antitumor compounds like purinyl pyridine and pyrimidine derivatives. Read More

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November 2021

Molecular adaptation response of Oenococcus oeni in non-Saccharomyces fermented wines: A comparative multi-omics approach.

Int J Food Microbiol 2021 Nov 20;362:109490. Epub 2021 Nov 20.

Universitat Rovira i Virgili, Departament de Bioquímica i Biotecnologia, Facultat d'Enologia, Grup de Biotecnologia Enològica, C/ Marcel·lí Domingo 1, 43007 Tarragona, Catalonia, Spain. Electronic address:

Oenococcus oeni is the main agent responsible for malolactic fermentation (MLF) in wine. This usually takes place in red wines after alcoholic fermentation (AF) carried out by Saccharomyces cerevisiae. In recent years, there is an increasing interest in using non-Saccharomyces yeast, usually in combination with S. Read More

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November 2021

2-((2-(4-Iodo-2,5-dimethoxyphenyl)ethylamino)methyl)phenol (25I-NBOH) and 2-(((2-(4-chloro-2,5-dimethoxyphenyl)ethyl)amino)methyl)phenol (25C-NBOH) induce adverse effects on the cardiovascular system.

Toxicol Lett 2021 Nov 26. Epub 2021 Nov 26.

National Institute of Food and Drug Safety Evaluation, Ministry of Food and Drug Safety, Osong, Cheongju, Republic of Korea. Electronic address:

Two new psychoactive substances (NPSs) classified as phenethylamines, namely 2-((2-(4-Iodo-2,5-dimethoxyphenyl)ethylamino)methyl)phenol (25I-NBOH) and 2-(((2-(4-chloro-2,5-dimethoxyphenyl)ethyl)amino)methyl)phenol (25C-NBOH), are being abused by people seeking recreational hallucinogens. These NPSs may cause serious health problems as their adverse effects are not known in most cases. Therefore, in the present study, we evaluated the cardiotoxicity of 25I-NBOH and 25C-NBOH using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, rat electrocardiography (ECG), Langendorff test, and human ether-a-go-go-related gene (hERG) assay. Read More

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November 2021

Coptisine: A natural plant inhibitor of ruminal bacterial urease screened by molecular docking.

Sci Total Environ 2021 Nov 26:151946. Epub 2021 Nov 26.

State Key Laboratory of Animal Nutrition, Institute of Animal Sciences, Chinese Academy of Agricultural Sciences, Beijing 100193, China. Electronic address:

Inhibition of ruminal bacterial urease activity could slow down the decomposition of urea to ammonia, which would lead to a decrease in urea synthesis in the liver and urea-N emission in the urine. In order to find a rumen bacterial urease specific inhibitor that is environmentally friendly, we used the homology model of rumen bacterial urease as the target to screen natural compounds from plants by molecular docking. The screening results showed that coptisine had the most potential to inhibit the activity of rumen bacterial urease with an IC of 2. Read More

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November 2021

Metabolomics reveals changes in metabolite profiles due to growth and metamorphosis during the ontogeny of the northern damselfly.

J Insect Physiol 2021 Nov 27;136:104341. Epub 2021 Nov 27.

Department of Chemistry, Umeå University, SE 90187 Umea, Sweden.

Many insects have complex life cycles where a drastic ontogenetic change happens between the larval stages and the adult stage, i.e. metamorphosis. Read More

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November 2021

Synthesis and dopamine receptor binding of dihydrexidine and SKF 38393 catecholamine-based analogues.

Amino Acids 2021 Nov 29. Epub 2021 Nov 29.

Laboratory of Fine Organic Chemistry, Department of Chemistry and Biochemistry, Faculty of Sciences and Technology of São Paulo State University, Presidente Prudente, São Paulo, 19060-900, Brazil.

Dopamine is an important neurotransmitter that regulates numerous essential functions, including cognition and voluntary movement. As such, it serves as an important scaffold for synthesis of novel analogues as part of drug development effort to obtain drugs for treatment of neurodegenerative diseases, such as Parkinson's disease. To that end, similarity search of the ZINC database based on two known dopamine-1 receptor (D1R) agonists, dihydrexidine (DHX) and SKF 38393, respectively, was used to predict novel chemical entities with potential binding to D1R. Read More

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November 2021

New Physical Hydrogels Based on Co-Assembling of FMOC-Amino Acids.

Gels 2021 Nov 12;7(4). Epub 2021 Nov 12.

"Petru Poni" Institute of Macromolecular Chemistry, 41-A Grigore Ghica Voda Alley, 700487 Iasi, Romania.

In the last years, physical hydrogels have been widely studied due to the characteristics of these structures, respectively the non-covalent interactions and the absence of other necessary components for the cross-linking processes. Low molecular weight gelators are a class of small molecules which form higher ordered structures through hydrogen bonding and π-π interactions. In this context it is known that the formation of hydrogels based on FMOC-amino acids is determined by the primary structures of amino acids and the secondary structure arrangement (alpha-helix or beta-sheet motifs). Read More

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November 2021