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In the present study, a new series of 1,2,3-triazole derivatives was synthesized via a click one-pot reaction. The synthesized compounds were found to be active during molecular docking studies against targeted protein 1T69 by using the Molecular Operating Environment (MOE) software. The designed and synthesized compounds were characterized by using FT-IR, H-NMR and LC-MS spectra. The synthesized triazole moieties were further screened for their α-amylase and α-glucosidase inhibitory activities. The preliminary activity analysis revealed that all the compounds showed good inhibition activity, ranging from moderate to high depending upon their structures and concentrations and compared to the standard drug acarbose. Both in silico and in vitro analysis indicated that the synthesized triazole molecules are potent for DM type-II. Out of all the compounds, compound K-1 showed the maximum antidiabetic activity with 87.01% and 99.17% inhibition at 800 µg/mL in the α-amylase and α-glucosidase inhibition assays, respectively. Therefore these triazoles may be further used as promising molecules for development of antidiabetic compounds.
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http://dx.doi.org/10.3390/molecules28073104 | DOI Listing |
J Org Chem
September 2025
College of Chemistry and Materials Science, Key Laboratory of Analytical Science and Technology of Hebei Province, and MOE Key Laboratory of Medicinal Chemistry and Molecular Diagnostics, Hebei University, Baoding 071002, Hebei, China.
In this work, the previously reported SeODR strategy was used successfully for the synthesis of bicyclic peptides (). with different rings bearing various thioether linkages were prepared through a one-pot reaction; 15 with satisfactory yields were achieved. Cross-linkers including xylylene dibromide (, 2,6-bis(bromomethyl)pyridine (, 4,4'-bis(bromomethyl)biphenyl (), 1,3-dichloroacetone (, and dichloro--tetrazine ( are all compatible with the SeODR approach used for deprotection of the S-acetamidomethyl (Acm) group in peptides.
View Article and Find Full Text PDFBeilstein J Org Chem
July 2025
Department of Chemical and Environmental Process Engineering, Faculty of Chemical Technology and Biotechnology, Budapest University of Technology and Economics, Műegyetem rkp. 3., H-1111, Budapest, Hungary.
It was demonstrated that Cyrene, as a biomass-originated polar aprotic solvent, could be utilized as an alternative reaction medium for one-pot copper(I)-catalyzed azide-alkyne cycloaddition (click or CuAAC) reactions, for the synthesis of various 1,2,3-triazoles under mild conditions. Nineteen products involving -substituted-4-phenyl-1-1,2,3- and 1-allyl-4-substituted-1-1,2,3-triazoles were synthesized under one-pot conditions and isolated with good to excellent yields (50-96%) and purity (>98%). The observed results represent an example that proves that biomass-derived safer solvents can be introduced into a synthetically important transformation exhibiting higher chemical and environmental safety.
View Article and Find Full Text PDFChemistryOpen
July 2025
Department of Organic Chemistry and Natural Products, Chemistry and Chemical Engineering Research Center of Iran, Tehran, 14968-13151, Iran.
A double aldol condensation-Michael addition-cyclization-double click reaction sequence is conducted in one pot for the synthesis of a novel series of tetrahydro-chromene derivatives anchored with dual triazole rings. The process is optimized primarily step by step under ultrasonic irradiation in a basic aqueous t-BuOH medium. The steps are then successfully combined into a four-component one-pot reaction using the optimum conditions, where the whole operation took less than 2 h to complete.
View Article and Find Full Text PDFNat Commun
July 2025
Organic Synthesis Group, Department of Organic and Macromolecular Chemistry, Faculty of Sciences, Ghent University, Ghent, Belgium.
Thiols are used in many click reactions, and are also excellent platforms for biomolecular click or bioconjugation reactions. The direct cross-coupling of two thiols is an attractive biomimetic concept for click chemistry, but leads to statistical mixtures of homo- and heterodimers. Here, we introduce a novel class of thiol-click reagents, bromo-ynones, where the kinetic differentiation between the first and second thiol addition onto these reagents facilitates a stepwise one-pot cross-clicking of two distinct thiols in aqueous media, without the need for intermediate isolation or purification.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
September 2025
Fachbereich Biologie, Chemie, Pharmazie Institut für Chemie und Biochemie - Anorganische Chemie Freie Universität Berlin, Fabeckstr. 34/36, 14195, Berlin, Germany.
Herein, the investigation of inorganic reagents containing the pentafluorooxosulfate (OSF) moiety is presented. First, the gram-scale preparation of the reactive yet stable pentafluorosulfur hypofluorite (FOSF) as well as its spectroscopic data are reported. Then, the preparation and full characterization of the corresponding fluorosulfonyl pentafluorooxosulfate (FSOSF, FSPO) by the fluoro-pentafluorooxosulfanylation of SO are highlighted.
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