Results 11 to 20 of about 7,707 (195)
1,2,3-Triazoles as Biomimetics in Peptide Science [PDF]
Molecules, 2021 Natural peptides are an important class of chemical mediators, essential for most vital processes. What limits the potential of the use of peptides as drugs is their low bioavailability and enzymatic degradation in vivo. To overcome this limitation, the development of new molecules mimicking peptides is of great importance for the development of new ...
Naima Agouram +2 more
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A practical flow synthesis of 1,2,3-triazoles
RSC Advances, 2022 Copper-on-charcoal is an excellent heterogeneous catalyst for the alkyne–azide cycloaddition reaction performed under continuous flow conditions. 2-Ynoic acids undergo decarboxylation/cycloaddition cascade giving triazoles bearing small alkyl chains.
Dawid Drelinkiewicz, Richard J. Whitby
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1,2,3-Triazole Derivatives as Novel Antifibrinolytic Drugs
International Journal of Molecular Sciences, 2022 Fibrinolysis is a natural process that ensures blood fluidity through the removal of fibrin deposits. However, excessive fibrinolytic activity can lead to complications in different circumstances, such as general surgery or severe trauma. The current antifibrinolytic drugs in the market, aminocaproic acid (EACA) and tranexamic acid (TXA), require high ...
Oriol Bosch-Sanz +7 more
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1,2,3-Triazoles and their metal chelates with antimicrobial activity
Frontiers in Chemistry, 2023 The emergence of drug-resistant bacterial and fungal pathogens has highlighted the urgent need of innovative antimicrobial therapeutics. Transition metal complexes with biologically active ligands (coumarins, terpyridines, triazoles, uracils, etc.) have long been investigated for antimicrobial activity.
Lozan Todorov, Irena Kostova
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Versatile Synthetic Platform for 1,2,3-Triazole Chemistry
ACS Omega, 2022 1,2,3-Triazole scaffolds are not obtained in nature, but they are still intensely investigated by synthetic chemists in various fields due to their excellent properties and green synthetic routes. This review will provide a library of all synthetic routes used in the past 21 years to synthesize 1,2,3-triazoles and their derivatives using various metal ...
Disha P. Vala +2 more
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Enzymatic Macrocyclization of 1,2,3‐Triazole Peptide Mimetics [PDF]
Angewandte Chemie International Edition, 2016 AbstractThe macrocyclization of linear peptides is very often accompanied by significant improvements in their stability and biological activity. Many strategies are available for their chemical macrocyclization, however, enzyme‐mediated methods remain of great interest in terms of synthetic utility.
Emilia Oueis +3 more
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Synthesis of Deuterated 1,2,3-Triazoles [PDF]
The Journal of Organic Chemistry, 2012 The copper-catalyzed azide-alkyne cycloaddition (CuAAC) is a highly effective method for the selective incorporation of deuterium atom into the C-5 position of the 1,2,3-triazole structure. Reactions of alkynes and azides can be conveniently carried out in a biphasic medium of CH(2)Cl(2)/D(2)O, using the CuSO(4)/Na ascorbate system. The mildness of the
Hari K. Akula, Mahesh K. Lakshman
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Regioselective Reduction of 1H-1,2,3-Triazole Diesters [PDF]
Molecules, 2021 Regioselective reactions can play pivotal roles in synthetic organic chemistry. The reduction of several 1-substituted 1,2,3-triazole 4,5-diesters by sodium borohydride has been found to be regioselective, with the C(5) ester groups being more reactive towards reduction than the C(4) ester groups.
Butler, Christopher R. +2 more
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Discovery of Novel 1,2,3-triazole Derivatives as IDO1 Inhibitors
Pharmaceuticals, 2022 Indoleamine 2,3-dioxygenase 1 (IDO1) has received much attention as an immunomodulatory enzyme in the field of cancer immunotherapy. While several IDO1 inhibitors have entered clinical trials, there are currently no IDO1 inhibitor drugs on the market. To explore potential IDO1 inhibitors, we designed a series of compounds with urea and 1,2,3-triazole ...
Xixi Hou +4 more
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Synthesis and antitumoral activity of novel biaryl hydroxy-triazole and fluorene-triazole hybrids [PDF]
Exploration of Drug ScienceAim: The development of selective and potent antitumor agents remains a significant challenge. This study aimed to synthesize and evaluate biaryl hydroxy-1,2,3-triazoles and 9H-fluorene-1,2,3-triazole hybrids, inspired by previously identified bioactive ...
David Chafi Zeitune +6 more
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