keyword
https://read.qxmd.com/read/38535256/water-soluble-quaternary-and-protonable-basic-chitotriazolans-synthesis-by-click-chemistry-conversion-of-chitosan-azides-and-investigation-of-antibacterial-activity
#1
JOURNAL ARTICLE
Sankar Rathinam, Romano Magdadaro, Martha Á Hjálmarsdóttir, Már Másson
The azide transfer reaction and copper(I)-catalyzed alkyne-azide cycloaddition (CuAAC) can be used to convert the amino groups in chitosan to triazole 1,2,3-moieties. The resulting polymer has been named chitotriazolan. This synthesis was performed with six different quaternary ammonium alkynes and three amine alkynes to obtain a series of nine water-soluble chitotriazolan derivatives. The structure and complete conversion of the azide were confirmed by FT-IR and proton NMR spectroscopy. The derivatives were investigated for antibacterial activity against S...
March 5, 2024: Journal of Functional Biomaterials
https://read.qxmd.com/read/38534143/triazole-resistance-in-aspergillus-fumigatu-s-isolated-from-a-tomato-production-environment-exposed-to-propiconazole
#2
JOURNAL ARTICLE
Alejandra M Jimenez Madrid, Raees A Paul, Francesca Rotondo, Loic Deblais, Gireesh Rajashekara, Sally A Miller, Melanie L Lewis Ivey
UNLABELLED: The emergence of azole-resistant Aspergillus fumigatus (AR Af ) across the world is an important public health concern. We sought to determine if propiconazole, a demethylase inhibitor (DMI) fungicide, exerted a selective pressure for AR Af in a tomato production environment following multiple exposures to the fungicide. A tomato field trial was established in 2019 and propiconazole was applied weekly until harvest. Soil, leaf, and fruit (when present) samples were collected at baseline and after each propiconazole application...
March 27, 2024: Applied and Environmental Microbiology
https://read.qxmd.com/read/38531546/bergofungin-d-a-peptaibol-template-for-the-introduction-of-chemical-modifications-synthesis-of-analogs-and-comparative-studies-of-their-structures
#3
JOURNAL ARTICLE
Sanjit Das, Khoubaib Haj Ben Salah, Emmanuel Wenger, Baptiste Legrand, Claude Didierjean, Nicolas Inguimbert
Bergofungin D is a helical peptide of the peptaibol family consisting of 14 amino acids, six of which are the helix inducer aminoisobutyric acid (Aib). In the second third of the sequence, a hydroxyproline causes a bending of the helix and a disruption of the hydrogen bond network, and Aib7 is the only amino acid in this region involved in the hydrogen bond network. Therefore, modification of this residue can serve as a probe to monitor the effect of introducing amino acid substitutions on this more fragile helical turn...
March 26, 2024: Journal of Peptide Science
https://read.qxmd.com/read/38530488/isolation-identification-and-transcriptome-analysis-of-triadimefon-degrading-strain-enterobacter-hormaechei-ty18
#4
JOURNAL ARTICLE
Yan Wang, Qi Guan, Wenhui Jiao, Jiangbo Li, Rui Zhao, Xiqian Zhang, Weixin Fan, Chunwei Wang
Triadimefon, a type of triazole systemic fungicide, has been extensively used to control various fungal diseases. However, triadimefon could lead to severe environmental pollution, and even threatens human health. To eliminate triadimefon residues, a triadimefon-degrading bacterial strain TY18 was isolated from a long-term polluted site and was identified as Enterobacter hormaechei. Strain TY18 could grow well in a carbon salt medium with triadimefon as the sole nitrogen source, and could efficiently degrade triadimefon...
March 26, 2024: Biodegradation
https://read.qxmd.com/read/38529572/a-series-of-isostructural-metal-organic-frameworks-for-an-enhanced-electro-catalytic-oxygen-evolution-reaction
#5
JOURNAL ARTICLE
Pampa Jhariat, Abdul Kareem, Priyanka Kumari, Shafeeq Sarfudeen, Premchand Panda, Sellappan Senthilkumar, Tamas Panda
Three new isostructural MOFs (ZnTIA, CoTIA and CdTIA) were synthesized by the solvothermal synthesis of the organic linker 5-triazole isophthalic acid (5-TIA) with the transition metals Zn(II), Co(II) and Cd(II) in the presence of the structure directing agent tetramethyl ammonium chloride (TMA). These three MOFs were characterized thoroughly by ScXRD, PXRD, FT-IR, TGA, BET and SEM. They have excellent thermal and water stabilities. Among all these MOFs mentioned, pristine CoTIA exhibited excellent electrocatalytic activity toward the oxygen evolution reaction (OER)...
March 26, 2024: Dalton Transactions: An International Journal of Inorganic Chemistry
https://read.qxmd.com/read/38529554/discovery-of-novel-acrylopimaric-acid-triazole-derivatives-as-promising-antifungal-agents
#6
JOURNAL ARTICLE
Xu Han, Renle Xu, Shihao Gu, Yue Kong, Yuhang Lou, Yanqing Gao, Shibin Shang, Zhanqian Song, Jie Song, Jian Li
BACKGROUND: To further develop potential natural fungicides, two series of new acrylopimaric acid triazole derivatives were synthesized, and their antifungal activities were tested and evaluated. RESULTS: In vitro antifungal activity results indicated that Compound 5m exhibited significant inhibitory activity against Rhizoctonia solani with an EC50 value of 1.528 mg/L. Its antifungal effect was comparable to that of the commercially available fungicide fluconazole, epoxiconazole and propiconazole (EC50 value of 1...
March 26, 2024: Pest Management Science
https://read.qxmd.com/read/38524479/new-benzimidazole-triazole-derivatives-as-topoisomerase-i-inhibitors-design-synthesis-anticancer-screening-and-molecular-modeling-studies
#7
JOURNAL ARTICLE
Ulviye Acar Çevik, Betül Kaya, Ismail Celik, Mithun Rudrapal, Gourav Rakshit, Arzu Karayel, Serkan Levent, Derya Osmaniye, Begüm Nurpelin Sağlık Özkan, Merve Baysal, Özlem Atlı Ekliog Lu, Yusuf Özkay, Zafer Asım Kaplancıklı
In this study, we designed, synthesized, and evaluated a series of 1,2,4-triazole benzimidazoles for their cytotoxic effects against the A549, C6, and NIH3T3 cell lines. Additionally, these compounds were assessed for their inhibitory activity against DNA topoisomerase I, aiming to develop novel anticancer agents. The synthesized final compounds 4a - h were characterized using 1 H NMR, 13 C NMR, and HRMS. Among them, compounds 4b and 4h emerged as the most potent agents against the A549 cell line, exhibiting an IC50 value of 7...
March 19, 2024: ACS Omega
https://read.qxmd.com/read/38524460/average-electron-density-a-quantitative-tool-for-evaluating-non-classical-bioisosteres-of-amides
#8
JOURNAL ARTICLE
Alaa Ma Osman, Alya A Arabi
Bioisosterism is strategically used in drug design to enhance the pharmacokinetic and pharmacodynamic properties of therapeutic molecules. The average electron density (AED) tool has been used in several studies to quantify similarities among nonclassical bioisosteres of carboxylic acid. In this study, the AED tool is used to quantify the similarities among nonclassical bioisosteres of an amide group. In particular, amide-to-1,2,3-triazole bioisosterism is considered. To evaluate the AED differences exhibited by isomers of nonclassical bioisosteres, both isomers of amide ( cis and trans ) and 1,2,3-triazole (1,4 and 1,5 disubstituted moieity) were considered...
March 19, 2024: ACS Omega
https://read.qxmd.com/read/38524233/in-response-to-nguyen-et-al-mold-active-triazole-prophylaxis-utilization-among-patients-with-acute-myeloid-leukemia-in-a-community-hospital
#9
JOURNAL ARTICLE
Michael J Williams, Margaret Cook, Brittany Mejaki, Brian P Buggy
No abstract text is available yet for this article.
March 2024: Open Forum Infectious Diseases
https://read.qxmd.com/read/38521876/1-2-3-triazole-and-chiral-schiff-base-hybrids-as-potential-anticancer-agents-dft-molecular-docking-and-adme-studies
#10
JOURNAL ARTICLE
Yonas Belay, Alfred Muller, Fanikie S Mokoena, Adedapo S Adeyinka, Lesetja R Motadi, Abel K Oyebamiji
A series of novel 1,2,3-triazole and chiral Schiff base hybrids 2-6 were synthesized by Schiff base condensation reaction from pre-prepared parent component of the hybrids (1,2,3-triazole 1) and series of primary chiral amines and their chemical structure were confirmed using NMR and FTIR spectroscopies, and CHN elemental analysis. Compounds 1-6 were evaluated for their anticancer activity against two cancer PC3 (prostate) and A375 (skin) and MRC-5 (healthy) cell lines by Almar Blue assay method. The compounds exhibited significant cytotoxicity against the tested cancer cell lines...
March 23, 2024: Scientific Reports
https://read.qxmd.com/read/38521013/synthesis-of-new-trypanocidal-agents-from-the-hybridisation-of-metronidazole-and-eugenol-analogues
#11
JOURNAL ARTICLE
Mônica Fraccarolli Pelozo, Cleydson Finotti Cordeiro, Letícia Fonseca Inácio, Rayssa de Cassia Alves Lemini, Elda Gonçalves Souza E Leite, Monique Dias Benedetti, Cristiane Alves Tulha, Rômulo Dias Novaes, Ivo Santana Caldas, Diogo Teixeira Carvalho, Stefânia Neiva Lavorato, Jamie Anthony Hawkes, Lucas Lopardi Franco
Nitroimidazole compounds are well-known bioactive substances, and the structural activity relationship has been reported whereby the position of the nitro group within the imidazole ring has a large influence on the activity. This study focuses on synthesising new trypanocidal agents from the hybridisation of metronidazole with different natural phenols (eugenol, dihydroeugenol and guaiacol). Two different coupling methodologies have been explored in order to analyse the influence of the connector on bioactivity: i) classic direct esterification (AD compounds) and ii) "click" chemistry using a triazole connector (AC compounds)...
March 15, 2024: Bioorganic Chemistry
https://read.qxmd.com/read/38521011/modular-preparation-of-biphenyl-triazoles-via-click-chemistry-as-non-competitive-hyaluronidase-inhibitors
#12
JOURNAL ARTICLE
Yiman Qin, Guanyi Li, Ling Wang, Guangyuan Yin, Xiang Zhang, Hongxiang Wang, Pengfei Zheng, Wentao Hua, Yan Cheng, Yaxue Zhao, Jiong Zhang
Hyaluronidase is a promising target in drug discovery, given its overexpression in a range of physiological and pathological processes, including tumor migration, skin aging, sagging, and wrinkling, as well as inflammation and bacterial infections. In this study, to identify novel hyaluronidase inhibitors, we applied click chemistry for the modular synthesis of 370 triazoles in 96-well plates, starting with biphenyl azide. Utilizing an optimized turbidimetric screening assay in microplates, we identified Fmoc-containing triazoles 5 and 6, as well as quinoline-containing triazoles 15 and 16, as highly effective hyaluronidase inhibitors...
March 16, 2024: Bioorganic Chemistry
https://read.qxmd.com/read/38516597/stereoselective-synthesis-and-antiproliferative-activity-of-allo-gibberic-acid-based-1-3-aminoalcohol-regioisomers
#13
JOURNAL ARTICLE
Zein Alabdeen Khdar, Tam Minh Le, Zsuzsanna Schelz, István Zupkó, Zsolt Szakonyi
A new library of allo -gibberic acid-based aminoalcohol regioisomers was synthesised stereoselectively starting from commercially available gibberellic acid, which yields allo -gibberic acid under mild acidic conditions. The successful formation of hydroxymethyl ketone derivative 5, by acid-mediated rearrangement of previously prepared epoxide, paved the way to obtain the desired 1,3-aminoalcohols through Schiff base formation. To obtain the desired regioisomers, the primary alcohol functionality of 5 was subjected to mesylation, then replaced with either primary amine or sodium azide...
March 20, 2024: RSC medicinal chemistry
https://read.qxmd.com/read/38516328/a-bifunctional-electrocatalyst-for-oer-and-orr-based-on-a-cobalt-ii-triazole-pyridine-bis-cobalt-iii-corrole-complex
#14
JOURNAL ARTICLE
Abdalaziz Aljabour, Houssein Awada, Luyang Song, He Sun, Simon Offenthaler, Farzaneh Yari, Matthias Bechmann, Markus Clark Scharber, Wolfgang Schöfberger
As alternative energy sources are essential to reach a climate-neutral economy, hydrogen peroxide (H2 O2 ) as futuristic energy carrier gains enormous awareness. However, seeking for stable and electrochemically selective H2 O2 ORR electrocatalyst is yet a challenge, making the design of-ideally-bifunctional catalysts extremely important and outmost of interest. In this study, we explore the application of a trimetallic cobalt(II) triazole pyridine bis-[cobalt(III) corrole] complex CoII TP[CoIII C]2 3 in OER and ORR catalysis due to its remarkable physicochemical properties, fast charge transfer kinetics, electrochemical reversibility, and durability...
May 15, 2023: Angewandte Chemie
https://read.qxmd.com/read/38513973/treatment-using-vanillin-derived-synthetic-molecules-incorporated-into-polymeric-micelles-is-effective-against-infection-caused-by-leishmania-amazonensis-species
#15
JOURNAL ARTICLE
Isabela A G Pereira, Camila S Freitas, Raquel S B Câmara, Marcelo M Jesus, Daniela P Lage, Grasiele S V Tavares, Tauane G Soyer, Fernanda F Ramos, Nícia P Soares, Samira S Santiago, Vívian T Martins, Danniele L Vale, Breno L Pimenta, Fernanda Ludolf, Fabrício M Oliveira, Mariana C Duarte, Miguel A Chávez-Fumagalli, Adilson V Costa, Denise U Gonçalves, Bruno M Roatt, Róbson R Teixeira, Eduardo A F Coelho
Treatment against leishmaniasis presents problems, mainly due to the toxicity of the drugs, high cost, and the emergence of resistant strains. A previous study showed that two vanillin-derived synthetic molecules, 3s [4-(2-hydroxy-3-(4-octyl-1H-1,2,3-triazol-1-yl)propoxy)-3-methoxybenzaldehyde] and 3t [4-(3-(4-decyl-1H-1,2,3-triazol-1-yl)-2-hydroxypropoxy)-3-methoxybenzaldehyde], presented antileishmanial activity against Leishmania infantum, L. amazonensis, and L. braziliensis species. In the present work, 3s and 3t were evaluated to treat L...
March 19, 2024: Experimental Parasitology
https://read.qxmd.com/read/38513646/flex-genetically-encodable-enzymatic-fluorescence-signal-amplification-using-engineered-peroxidase
#16
JOURNAL ARTICLE
Nirmali Sharma, Minkyo Jung, Pratyush Kumar Mishra, Ji Young Mun, Hyun-Woo Rhee
Fluorescent tagging of biomolecules enables their sensitive detection during separation and determining their subcellular location. In this context, peroxidase-based reactions are actively utilized for signal amplification. To harness this potential, we developed a genetically encodable enzymatic fluorescence signal amplification method using APEX (FLEX). We synthesized a fluorescent probe, Jenfluor triazole (JFT1), which effectively amplifies and restricts fluorescence signals under fixed conditions, enabling fluorescence-based detection of subcellularly localized electron-rich metabolites...
March 8, 2024: Cell Chemical Biology
https://read.qxmd.com/read/38513073/potent-inhibition-of-e-coli-dxp-synthase-by-a-gem-diaryl-bisubstrate-analog
#17
JOURNAL ARTICLE
Lauren B Coco, Eucolona M Toci, Percival Yang-Ting Chen, Catherine L Drennan, Caren L Freel Meyers
New antimicrobial strategies are needed to address pathogen resistance to currently used antibiotics. Bacterial central metabolism is a promising target space for the development of agents that selectively target bacterial pathogens. 1-Deoxy-d-xylulose 5-phosphate synthase (DXPS) converts pyruvate and d-glyceraldehyde 3-phosphate (d-GAP) to DXP, which is required for synthesis of essential vitamins and isoprenoids in bacterial pathogens. Thus, DXPS is a promising antimicrobial target. Toward this goal, our lab has demonstrated selective inhibition of Escherichia coli DXPS by alkyl acetylphosphonate (alkylAP)-based bisubstrate analogs that exploit the requirement for ternary complex formation in the DXPS mechanism...
March 21, 2024: ACS Infectious Diseases
https://read.qxmd.com/read/38512800/stereochemical-and-computational-nmr-survey-of-1-2-3-triazoles-in-search-of-the-original-tauto-conformers
#18
JOURNAL ARTICLE
Valentin A Semenov, Lyudmila I Larina
The conformational analysis of nine functionalized 1,2,3-triazoles was carried out by the correlation of calculated and experimental high-level nuclear magnetic resonance (NMR) chemical shifts. In solution, the studied triazoles are in exchange dynamic equilibrium caused by their prototropic tautomerism of the NH-proton. The experimentally unresolved NMR signals were assigned for most of the compounds. A more thorough survey was conducted for 4- t -butyl-1,2,3-triazole-5-carbaldehyde oxime. The analysis performed within the framework of the DP4+ formalism completely confirmed the hypothesis of the predominance of the 2H-tautomer...
March 21, 2024: Journal of Physical Chemistry. A
https://read.qxmd.com/read/38511836/synthesis-and-application-of-task-specific-bimetal-organic-frameworks-in-the-synthesis-of-biological-active-spiro-oxindoles
#19
JOURNAL ARTICLE
Elham Tavakoli, Hassan Sepehrmansourie, Mohammad Ali Zolfigol, Ardeshir Khazaei, Abdolmajid Mohammadzadeh, Elaheh Ghytasranjbar, Mohammad Ali As'Habi
The use of click chemistry as a smart and suitable method for the development of new heterogeneous catalysts is based on metal-organic frameworks as well as the production of organic compounds. The development of the click chemistry method can provide a new strategy to achieve superior properties of MOFs. Here, the two metals Co and Fe are used to create a bimetallic-organic framework. In the following, the click chemistry and postmodification method are well organized and an acidic heterogeneous porous catalyst is developed...
March 21, 2024: Inorganic Chemistry
https://read.qxmd.com/read/38509452/asymmetric-synthesis-of-triazole-antifungal-agents-enabled-by-an-upgraded-strategy-for-the-key-epoxide-intermediate
#20
JOURNAL ARTICLE
Yu Tang, Zhuo Li, Meiqi Zeng, Ran Li, Hao Song, Dan Zhang, Fei Xue, Yong Qin
A streamlined and efficient approach to the key epoxide intermediate for the asymmetric synthesis of triazole antifungal agents is presented. This synthesis highlights a P(NMe2 )3 -mediated nonylidic olefination of α-keto ester, ensuring the exclusive formation of the requisite ( Z )-alkene, followed by a highly enantioselective Jacobsen epoxidation to establish the two vicinal stereocenters in a single step. The versatility of this strategy is exemplified through the efficient synthesis of efinaconazole and ravuconazole...
March 20, 2024: Journal of Organic Chemistry
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