New click-chemistry methods for 1, 2, 3-triazoles synthesis: Recent advances and applications
J Totobenazara, AJ Burke - Tetrahedron letters, 2015 - Elsevier
Triazoles find applications in several major technological areas, and especially in drug
discovery. The click-chemistry approaches based on Huisgen's cycloaddition reaction are …
discovery. The click-chemistry approaches based on Huisgen's cycloaddition reaction are …
Click chemistry-aided drug discovery: A retrospective and prospective outlook
R Zhao, J Zhu, X Jiang, R Bai - European Journal of Medicinal Chemistry, 2024 - Elsevier
Click chemistry has emerged as a valuable tool for rapid compound synthesis, presenting
notable advantages and convenience in the exploration of potential drug candidates. In …
notable advantages and convenience in the exploration of potential drug candidates. In …
Mechanistic applications of click chemistry for pharmaceutical drug discovery and drug delivery
Highlights•Basic mechanism for all the discussed click reaction has been shown.•Many new
enzyme inhibitors was identified by drug discovery using click approaches.•Drug delivery by …
enzyme inhibitors was identified by drug discovery using click approaches.•Drug delivery by …
Development of potent inhibitors by fragment‐linking strategies
EV Bedwell, WJ McCarthy, AG Coyne… - Chemical Biology & …, 2022 - Wiley Online Library
Fragment‐based drug discovery (FBDD) is a method of identifying small molecule hits that
can be elaborated rationally through fragment growing, merging and linking, to afford high …
can be elaborated rationally through fragment growing, merging and linking, to afford high …
Target‐directed azide‐alkyne cycloaddition for assembling HIV‐1 TAR RNA binding ligands
The highly conserved HIV‐1 transactivation response element (TAR) binds to the trans‐
activator protein Tat and facilitates viral replication in its latent state. The inhibition of Tat …
activator protein Tat and facilitates viral replication in its latent state. The inhibition of Tat …
Kinetic target-guided synthesis: reaching the age of maturity: miniperspective
D Bosc, V Camberlein, R Gealageas… - Journal of Medicinal …, 2019 - ACS Publications
Kinetic target-guided synthesis (KTGS) is an original discovery strategy allowing a target to
catalyze the irreversible synthesis of its own ligands from a pool of reagents. Although …
catalyze the irreversible synthesis of its own ligands from a pool of reagents. Although …
Kinetic target-guided synthesis in drug discovery and chemical biology: a comprehensive facts and figures survey
For the last 15 years, kinetic target-guided syntheses, including in situ click chemistry, have
been used as alternative methods to find ligands to therapeutically relevant proteins. In this …
been used as alternative methods to find ligands to therapeutically relevant proteins. In this …
New insights into the kinetic target-guided synthesis of protein ligands
The kinetic target-guided synthesis (KTGS) strategy is an unconventional discovery
approach that takes advantage of the presence of the biological target itself in order to …
approach that takes advantage of the presence of the biological target itself in order to …
Tailored bioorthogonal and bioconjugate chemistry: a source of inspiration for developing kinetic target-guided synthesis strategies
Kinetic target-guided synthesis (KTGS) is a promising tool for the discovery of biologically
active compounds. It relies on the identification of potent ligands that are covalently …
active compounds. It relies on the identification of potent ligands that are covalently …
Design, synthesis and biological evaluation of N-methyl-N-[(1, 2, 3-triazol-4-yl) alkyl] propargylamines as novel monoamine oxidase B inhibitors
O Di Pietro, N Alencar, G Esteban, E Viayna… - Bioorganic & medicinal …, 2016 - Elsevier
Different azides and alkynes have been coupled via Cu-catalyzed 1, 3-dipolar Huisgen
cycloaddition to afford a novel family of N 1-and C 5-substituted 1, 2, 3-triazole derivatives …
cycloaddition to afford a novel family of N 1-and C 5-substituted 1, 2, 3-triazole derivatives …