950984-75-5

Upstream product

• 6959-47-3 2-chloromethylpyridine hydrochloride 
• 2450-71-7 Propargylamine 
• 1539-42-0 bis[(2-pyridyl)methyl]amine 
• 106-96-7 propargyl bromide 
• 1121-60-4 pyridine-2-carbaldehyde 
• 3731-51-9 2-(Aminomethyl)pyridine 
• 4377-33-7 2-chloromethylpyridine 
• 119715-60-5 N-(2-pyridylmethyl)-2-pyridylmethanimine 

Downstream Products

• 1192206-14-6 C₂₂H₂₂N₆O 
• 1356371-36-2 C₅₈H₅₂N₁₂ 
• 1225579-76-9 C₂₁H₂₀N₆ 
• 1546975-40-9 1-(3-phenylisoxazol-5-yl)-N,N-bis(pyridin-2-ylmethyl)methanamine 
• 1567833-49-1 C₇₅H₁₀₂N₂₄O₁₃S 

Relevant academic research and scientific papers

Synthesis of DPA-triazole structures and their application as ligand for metal catalyzed organic reactions

In this work, the use of DPA-triazole (DPA = dipicolylamine) molecules as ligands for metal catalyzed organic reactions has been investigated. A small library of ligands has been prepared by a CuAAC (click reaction) between propargyl-DPA and different azi

Fluconazole analogues with metal-binding motifs impact metal-dependent processes and demonstrate antifungal activity in Candida albicans

Abstract: Azole antifungals are an important class of antifungal drugs due to their low cost, ability to be administered orally, and broad-spectrum activity. However, their widespread and long-term use have given rise to adaptation mechanisms that render these compounds less effective against common fungal pathogens, including Candida albicans. New antifungals are desperately needed as drug-resistant strains become more prevalent. We recently showed that copper supplementation potentiates the activity of the azole antifungal fluconazole against the opportunistic fungal pathogen C. albicans. Here, we report eight new azole analogues derived from fluconazole in which one triazole group has been replaced with a metal-binding group, a strategy designed to enhance potentiation of azole antifungal activity by copper. The bioactivity of all eight compounds was tested and compared to that of fluconazole. Three of the analogues showed activity against C. albicans and two had lower levels of trailing growth. One compound, Flu-TSCZ, was found to impact the levels, speciation, and bioavailability of cellular metals. Graphic abstract: [Figure not available: see fulltext.]

Molecular Recognition by Zn(II)-Capped Dynamic Foldamers

Two α-aminoisobutyric acid (Aib) foldamers bearing Zn(II)-chelating N-termini have been synthesized and compared with a reported Aib foldamer that has a bis(quinolinyl)/mono(pyridyl) cap (BQPA group). Replacement of the quinolinyl arms of the BQPA-capped foldamer with pyridyl gave a BPPA-capped foldamer, then further replacement of the linking pyridyl with a 1,2,3-triazole gave a BPTA-capped foldamer. Their ability to relay chiral information from carboxylate bound to Zn(II) at the N-terminus to a glycinamide-based NMR reporter of conformational preference at the C-terminus was measured. The importance of the quinolinyl arms became readily apparent, as the foldamers with pyridyl arms were unable to report on the presence of chiral carboxylate in acetonitrile. Low solubility, X-ray crystallography and 1H NMR spectroscopy suggested that interfoldamer interactions inhibited carboxylate binding. However changing solvent to methanol revealed that the end-to-end relay of chiral information could be observed for the Zn(II) complex of the BPTA-capped foldamer at low temperature.

An alternative modular 'click-SNAr-click' approach to develop subcellular localised fluorescent probes to image mobile Zn2+

Zn2+ is involved in a number of biological processes and its wide-ranging roles at the subcellular level, especially in specific organelles, have not yet been fully established due to a lack of tools to image it effectively. We report a new and

Ligand, preparation method thereof, fluorescent probe, and preparation method and application of fluorescent probe

The invention discloses a preparation method of a ligand, a fluorescent probe, and a preparation method and an application of the fluorescent probe. The ligand is DATP, and is obtained by reacting a compound 1, NaN3, tetrabutylammonium hydrogen sulfate, bis(2-pyridylmethyl)amine, propargyl bromide, CuI, and a CH2Cl2 and CF3COOH mixed solvent. The fluorescent probe adopts DATP and Ni as cores,Eu and Ni are linked with the ligand through a Ni-N coordination bond, and Tb is linked with the ligand trough Tb-O and Tb-N coordination bonds. The fluorescent probe of the invention is prepared with DATP as the core, and a Eu/Tb complex can be used in time-resolved fluorescence detection to effectively eliminate interference from samples and short-lived fluorescence such as scattered light, so the prepared fluorescent probe has the advantages of good water solubility, extremely high sensitivity, excellent selectivity to histidine, simple preparation method and mild conditions, and is suitable for detecting histidine in biological systems.

A bioinspired heterogeneous catalyst based on the model of the manganese-dependent dioxygenase for selective oxidation using dioxygen

A hybrid bioinspired material with manganese(ii) complexes grafted on the surface of a mesostructured porous silica is investigated. The Mn sites mimic the manganese-dependent dioxygenase (MndD), which is an enzyme that catalyses the oxidation of catechol derivatives. The metal complexes were introduced in the silica using a dinuclear complex [Mn2L2(Cl)2(μ-Cl)2] as a precursor with a clickable ligand N,N′-bis[(pyridin-2-yl)methyl]prop-2-yn-1-amine (L). Azide moieties covalently grafted on MCM-41 type mesoporous silica were utilised to anchor the manganese complex through Huisgen cycloaddition using CuBr(PPh3)3 as a catalyst. A second functional group-trimethylsilyl or pyridine—was grafted on the silica to bring, together with nanopore size confinement, a similar metal environment as in MndD. The mesostructure of the materials was maintained after incorporation of the Mn complex. Catalytic oxidation of 3,5-di-t-butyl-catechol (3,5-DTBC) into quinone occurred without the need of an additional base when the metal complex was confined in the porous solid. In comparision, the oxidation of 4-t-butyl-catechol (4-TBC) that always required a basic media led to a total oxidation into the ortho-quinone, contrary to the molecular analogue.

Alkane oxidation catalysed by a self-folded multi-iron complex

A preorganised ligand scaffold is capable of coordinating multiple Fe(II) centres to form an electrophilic CH oxidation catalyst. This catalyst oxidises unactivated hydrocarbons including simple, linear alkanes under mild conditions in good yields with selectivity for the oxidation of secondary CH bonds. Control complexes containing a single metal centre are incapable of oxidising unstrained linear hydrocarbons, indicating that participation of multiple centres aids the CH oxidation of challenging substrates.

Surfactant-modulated discriminative sensing of HNO and H2S with a Cu2+-complex-based fluorescent probe

Recent investigations revealed the close relationship between H2S and HNO in biological systems. It is significant to develop an efficient fluorescent sensor to realize the discriminative sensing of HNO and H2S. Herein, we designed and synthesized a novel fluorescent sensor (CuHCD) with hemicyanine-carbazole as fluorophore and bipyridine-triazole-Cu2+complex as receptor, which enabled the selective recognition of HNO and H2S, respectively via the non-covalent modulation of surfactant assemblies. The CuHCD/surfactant sensor system exhibited excellent selectivity for H2S at 5?mM SDS in HEPES buffer, and displayed high specificity for HNO at 1?mM SDS in HEPES buffer over other common anions and reactive species. Different detection mechanisms in sensing H2S and HNO were deeply investigated. The results showed that H2S seized Cu2+from the complex to recover the fluorescence of HCD, while HNO reduced Cu2+to Cu+in the complex to turn on the fluorescence. In different SDS micellar systems, HCD possessed different dispersity and binding capacity with Cu2+, which led to the selective detection of H2S and HNO, respectively. The hypothesis was further confirmed by replacing SDS micelles with liposome under the same conditions.

Copper-catalyzed regioselective hydroboration of terminal alkynes in aqueous medium

A mild and environment-friendly copper-catalyzed hydroboration of terminal alkynes in aqueous medium was reported. Regioselectivity control was achieved in the presence of cyclodextrin-bispyridine ligand (CD-1). This protocol was successfully applied to inactivated terminal alkynes. Moreover, the ligand was recovered and reused without any loss of activity over five cycles.

DENDRIMER COMPOSITIONS, METHODS OF SYNTHESIS, AND USES THEREOF

The disclosure relates to novel dendrimer conjugates and the methods of synthesizing the same, as well as systems and methods utilizing the dendrimer conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease diagnosis and/or therapy, etc.))).