Themed collection A Decade of Progress in Click Reactions Based on CuAAC

An ultrasound assisted CuAAC method afforded novel 1,2,3-triazoles derived from olanzapine as inhibitors of PDE4B.

A novel pharmacophore for apoptosis has been identified via a screening strategy in zebrafish.

We report a [3+2] cycloaddition using 3,6-bis-propargyloxy-1,2,4,5-tetrazine and azides to synthesize energetic polymers containing 1,2,4,5-tetrazine within the scaffold.

Exploring influenza neuraminidase inhibitors by targeting the charged residues near the entrance of the 150-cavity.

Copper-promoted azide/alkyne cycloadditions (CuAAC) are explored as a tool for modular introduction of peroxides onto molecules and nanomaterials.

The Cu(II)-alginate-based superporous hydrogel was prepared and used as a heterogenous catalyst in the regioselective click of 1,4-disubstituted-1,2,3-triazoles by CuAAC reactions.

A series of multi-target natural product-pyridoxine based derivatives were designed, synthesized, characterized and evaluated as anti-Alzheimer agents. Out of all the molecules of the series, 5i was found to be best.

Coumarin-based 1,4-disubstituted 1,2,3-triazole derivatives were synthesized using a highly efficient, eco-friendly protocol via a copper(I)-catalyzed click reaction between various substituted arylazides and terminal alkynes.

The present study involves development of novel quinoline triazole-containing cysteine protease inhibitors which arrest the development of P. falciparum at the trophozoite stage.

The fast and stable adsorption of modified PLL on activated surfaces was combined with the versatile catalyst-free click chemistry for the fast and selective functionalization of substrates with DNA.

Novel phenylalanine derivatives were discovered as HIV-1 capsid protein inhibitors via “click reaction”. Most of them exhibited remarkable anti-HIV-1 activity.

A facile, highly efficient, and greener method for the synthesis of new 1,4-disubstituted-1,2,3-triazoles was conducted using [Et₃NH][OAc] as a medium by the implementation of ultrasound irradiation via click chemistry, affording excellent yields.

A new self-stratified contact-killing antimicrobial polyurethane was synthesized via efficient and orthogonal click-chemistry.

A carbonylative Sonogashira coupling approach to the synthesis of glyco-alkynones is described.

The retaining β-glucosidase acid/base mutant TxGH116D593A catalyzed the production of 1-azido-β-D-glucose for synthesis of 15 1,2,3-triazole β-glucosyl derivatives.

A solvent-free process is described for the synthesis of tailor-made molecules from a one-pot, two-step approach combining aza-Michael addition and photoinduced copper(I) catalysed azide–alkyne (photo-CuAAC) reactions.

A novel 1,2,3-triazole furocoumarin derivatives with anti-vitiligo activity were synthesized via click chemistry.

We synthesized a carbohydrate-conjugated 4-(1,3,2-dithiarsolan-2-yl)aniline. It exhibited reduced cytotoxicity to normal cells, suggesting a feasible approach to improve the therapeutic index of arsenic-containing compounds as chemotherapeutic agents.

Cu(II) coordination polymers as photocatalysts for the copper-catalyzed azide–alkyne cycloaddition click reaction under household light irradiation in air.

Structurally related triazolic dendrimers were efficiently synthesized applying CuAAC reaction.

Glycals react with PIFA (or PIDA)–TMSN₃ in presence of TMSOTf to form sugar derived 1,2-diazides and vicinal azidoacetates. Synthesis of 2-azido-N-glycopeptides, pseudotrisaccharides, and a piperidine triol derivative is reported.

A novel alkyne-terminated cubic-octameric POSS was synthesised in high yield and click chemistry has been used to attach bio-oligomers.

A combination of flow chemistry and batch-based synthetic procedures has been successfully applied to the assembly of novel 4,5-unsaturated L-ascorbic acid series 6a–6n with diverse C-6-substituted 1,2,3-triazole moiety.

A protocol for the synthesis of 1,4-disubstituted 1,2,3-triazoles via three-component reaction by a water soluble copper(I) complex has been developed.

Microdroplets surface engineering using an azide fluorosurfactant prone to react with various functional heads conjugated beforehand to a strained alkyne.

Optimized polymer membrane surface modification with antimicrobial properties.

We have synthesized, via click-chemistry, a redox-active peptide–gallol conjugate which facilitates rapid formation of antimicrobial silver nanoparticles with prominent antifungal activity.

Drug entities able to address multiple targets can be more effective than those directed to just one biological target.

The Cu(II)/Tao-Phos-catalyzed Huisgen cycloaddition of succinimide-derived bisalkynes resulted in chiral triazoles bearing a quaternary carbon-stereogenic center with good yields and chemoselectivity as well as moderate to high enantioselectivities (up to 97% ee).

Synthesized benzimidazole based 1,3,4-oxadiazole-1,2,3-triazole conjugates were found to inhibit GSK-3β activity in vitro and exhibit antidepressant-like activity in in vivo studies.

We designed and synthesized a novel series of P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) inhibitors bearing a triazolphenethyl–tetrahydroisoquinoline scaffold through click chemistry.

Optimal binding mode of novel E. coli PDHc E1 inhibitor 9d.

A series of novel multifunctional polyacetylenes bearing oxadiazole and azo groups as molecular pendants were designed and synthesized via highly effective click chemistry.

A simple and enzyme-free lateral flow biosensor for the rapid detection of Cu²⁺ based on copper(I) ion (Cu⁺)-catalyzed click chemistry has been constructed for the first time.

In the present work we report on the click synthesis of a new camptothecin (CPT) prodrug based on an anionic polyamidoamine (PAMAM) dendrimer intended for cancer therapy.

Owing to its large surface area and rapid cellular uptake, graphene oxide (GO) is emerging as an attractive candidate material for delivery of drugs and genes.

Novel D–π–A–π–D type chromophores – 2,4-bis(4-aryl-1,2,3-triazol-1-yl)pyrrolo[2,3-d]pyrimidines were prepared and their photophysical, electrochemical properties in conjunction with quantum chemical calculations were investigated.

Two series of 3–12 multiarm star polymers and 4-miktoarm star copolymer of butadiene and styrene, in which the M_n of arm was higher than 20 kg mol⁻¹, were synthesized with high efficiency (from 85.0% to 96.1%) via click chemistry.

Herein we developed a functionalizable OFF–ON red emitting fluorescent calcium probe based on a new chelating system formed by CuAAC click chemistry (Huisgen cycloaddition).

The development of a microfluidic “click chip” incorporating an immobilized Cu(I) catalyst for click reactions.

2-Pyrrolecarbaldiminato–Cu(II) complexes were first established as efficient catalyst for 1,4-disubstituted 1,2,3-triazoles synthesis under green and mild reaction conditions.

Reactivity of ruthenium-catalyzed click reaction has been enhanced greatly by using H₂O as the solvent.

A novel magnetic heterogeneous copper catalyst was synthesized by immobilization of copper ions onto triazole functionalized Fe₃O₄.

Well-defined poly(N-(2-hydroxypropyl) methacrylamide) (PHPMA) was grafted onto graphene sheets via click chemistry to afford a PHPMA/graphene nanocomposite with excellent dispersibility in organic solvents and water.

We provide a convenient method to construct photo-responsive poly(carbonate)s via ring-opening polymerization of cyclic carbonates followed by azide–alkyne click chemistry.

A graphene oxide based ternary composite was synthesized for targeted drug carrier.

Conducting polyaniline nanofiber-grafted graphene oxide (PANINF-GO) hybrids were prepared by click chemistry reaction and in situ rapid mixing polymerization. The resulting composites exhibited excellent electrochemical properties.

A new family of triazolyl thiiranes has been synthesised and characterised as MMP-2 and MMP-9 inhibitors. The hit compound displayed submicromolar inhibition of MMP-2

A range of triazole-linked O-xylosides and O-xylobiosides, with potential biological applications, has been prepared by an efficient two-step chemoenzymatic sequence from biomass-derived xylans.

Efficient copper-catalyzed three-component synthesis of glycosylated iminocoumarins and 3-triazolyl-2-iminocoumarins.

Post assembly peptide modifications – serine/threonine kinase inhibitors.

Methodology and synthesis of different m₃G-CAP constructs equipped with an azide handle and their attachment by “click reaction” with an activated triple bond partner allows efficient formation of oligonucleotide m₃G-CAP conjugates.