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 …

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 …

Mechanistic applications of click chemistry for pharmaceutical drug discovery and drug delivery

NM Meghani, HH Amin, BJ Lee - Drug Discovery Today, 2017 - Elsevier
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 …

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 …

Target‐directed azide‐alkyne cycloaddition for assembling HIV‐1 TAR RNA binding ligands

R Paul, D Dutta, R Paul, J Dash - Angewandte Chemie, 2020 - Wiley Online Library
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 …

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 …

Kinetic target-guided synthesis in drug discovery and chemical biology: a comprehensive facts and figures survey

D Bosc, J Jakhlal, B Deprez… - Future Medicinal …, 2016 - Taylor & Francis
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 …

New insights into the kinetic target-guided synthesis of protein ligands

E Oueis, C Sabot, PY Renard - Chemical Communications, 2015 - pubs.rsc.org
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 …

Tailored bioorthogonal and bioconjugate chemistry: a source of inspiration for developing kinetic target-guided synthesis strategies

A Lossouarn, PY Renard, C Sabot - Bioconjugate Chemistry, 2020 - ACS Publications
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 …

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 …