J. Appl. Cryst.の発刊に際して

1,3,4-Thiadiazole: Synthesis, Reactions, and Applications in Medicinal, Agricultural, and Materials Chemistry

Dendrimers, which are highly branched, multivalent and monodisperse polymers, have received continuous interest in recent years because of the global demand for new nanomolecules that are useful in advanced technology and medicine. While dendrimers are advantageous for many highly specialised applications, the high polyvalency of higher-generation dendrimers requires, however, well-controlled, target-tailored regioselective chemical engineering. The structural evolution of dendrimers – from simple, monofunctional molecules to the more complex, multifunctional compounds – is inextricably associated with a continuous improvement in traditional synthetic strategies, as well as the development of new synthetic tools. The purpose of this review is to provide insight into currently available synthetic methods that yield dendrimers with various morphologies, placing emphasis on the evaluation of their advantages and limitations. In particular, we will review current efforts that focus on simplifying and optimising the existing methods and the development of new strategies that permit control over the targeted introduction of various functionalities in one or more selected areas of the molecule.

Advances in the chemistry of dendrimers

Comprehensive review on the anti-bacterial activity of 1,2,3-triazole hybrids.

Mixed self-assembly of ligands 1, 2, 1,6-hexanediamine (HDA), and Pd(NO3)2 afforded Fujita-type metal organic polyhedron MOP1 (diameter ≈ 8.2 nm), which is covalently functionalized with an average of 18 cucurbit[7]uril (CB[7]) units, as evidenced by 1H NMR, diffusion-ordered spectroscopy NMR, and transmission electron microscopy measurements. By virtue of the host–guest properties of CB[7], the inner cavity of MOP can be rendered hydrophobic by using octadecyl HDA (3) as guest during the self-assembly process. The hydrophobic cavity was successfully utilized to trap the hydrophobic dye Nile Red (NR) and the anticancer drug doxorubicin (DOX). The stimuli-responsive release of encapsulated NR or DOX occurs (1) upon addition of a competitive binder (e.g., adamantane ammonium (ADA)) for CB[7], (2) by a dual pH–chemical stimulus involving the protonation state change of adamantane carboxylate at pH 5.8, and (3) by a dual pH–photochemical stimulus involving photoisomerization of trans-6 to cis-6 at pH 5.8. NR ...

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Cucurbit[7]uril Enables Multi-Stimuli-Responsive Release from the Self-Assembled Hydrophobic Phase of a Metal Organic Polyhedron

Photophysical properties and dye-sensitized solar cell studies on thiadiazole–triazole–chalcone dendrimers

Chemical proteomics relies primarily on click-chemistry-based protein labeling and biotin-streptavidin enrichment, but these techniques have inherent limitations. Enrichment of intracellular proteins using a totally synthetic host-guest complex is described, overcoming the problem associated with the classical approach. We achieve this by affinity-based protein labeling with a target-specific probe molecule conjugated to a high-affinity guest (suberanilohydroxamic acid-ammonium-adamantane; SAHA-Ad) and then enriching the labeled species using a cucurbit[7]uril bead. This method shows high specificity for labeled molecules in a MDA-MB-231 breast cancer cell lysate. Moreover, this method shows promise for labeling proteins in live cells.

Enrichment of Specifically Labeled Proteins by an Immobilized Host Molecule

S-BINOL based chiral dendrimers with m-terphenyl at the surface and triazole as the bridging unit have been synthesized by a convergent synthetic strategy through the ‘click’ chemistry approach. The resazurin reduction assay method shows that all the dendrimers exhibit antibacterial activity against Shigella dysenteriae, Staphylococcus aureus and Serratia marcescen. Dendrimer 2 shows better inhibitory activity than dendrimers 1 and 3 towards Shigella dysenteriae and Staphylococcus aureus and the antibacterial activity of dendrimer 2 is comparable to that of the standard viz., streptomycin. Further molecular docking studies also supported our results.

Synthesis of chiral core based triazole dendrimers with m-terphenyl surface unit and their antibacterial studies

The mol­ecule of the title chalcone derivative, C21H20O5, consists of two substituted aromatic rings bridged by a prop-2-en-1-one group. The dihedral angle between the two benzene rings is 28.7 (7)°. In the crystal, mol­ecules are linked into C(10) chains running along the a axis by inter­molecular C—H⋯O hydrogen bonds, and the chains are cross-linked via C—H⋯π inter­actions.

https://journals.iucr.org/e/issues/2010/09/00/bt5297/bt5297.pdf

(E)-1-[4-(Prop-2-yn-1-yl-oxy)phen-yl]-3-(3,4,5-trimeth-oxy-phen-yl)prop-2-en-1-one.

A series of novel dendrimers with pyrrolidine as surfacegroup has been achieved in high yields by terminal-group modifica-tion on chalcone dendrimers through the application of 1,3-dipolarcycloaddition reaction. In 1,3-dipolar cycloaddition, azomethineylides (AMY) with alkenes afforded five-membered N -methyl pyr-rolidine. The formation of N -methyl pyrrolidine in the dendriticstructure would be an important candidate in the field of biologyand pharmacology. Key words: dendrimer, pyrrolidine, chalcone, 1,3-dipolar cycload-dition Design and synthesis of dendritic architectures have beenactive areas of research because of their countless applica-tions in the field of biology and material sciences. 1–4 Den-drimers are highly branched, regularly orderedmonodisperse three-dimensional architecture. The combi-nation of discrete numbers of functionalities and high lo-cal densities of active groups in dendrimers has attracteda lot of attention from those active in medicinal chemis-try.

Ayyavu Thirunarayanan

Papers

Photophysical properties and dye-sensitized solar cell studies on thiadiazole–triazole–chalcone dendrimers

Enrichment of Specifically Labeled Proteins by an Immobilized Host Molecule

Synthesis of chiral core based triazole dendrimers with m-terphenyl surface unit and their antibacterial studies

(E)-1-[4-(Prop-2-yn-1-yl-oxy)phen-yl]-3-(3,4,5-trimeth-oxy-phen-yl)prop-2-en-1-one.

A Facile Synthesis of Novel Pyrrolidine Dendrimers by Terminal Group Modification through 1,3-Dipolar Cycloaddition Reaction