Fully synthetic medium-sized macrocyclic peptides mimicking the key β-hairpin and α-helical protein epitopes relevant in many protein-protein interactions have emerged as a novel class of drugs with the potential to fill an important gap between small molecules and proteins. Conformationally stabilized macrocyclic scaffolds represent ideal templates for medicinal chemists to incorporate bioacti...

The Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC, known as the click reaction) is an established tool used for the construction of complex molecular architectures. Given its efficiency it has been widely applied for bioconjugation, polymer and dendrimer synthesis. More recently, this reaction has been utilized for the efficient formation of rigid or shape-persistent, preorganized macrocycl...

Macrocyclic trichothecenes, mycotoxins produced by Stachybotrys chartarum, have been implicated in adverse reactions in individuals exposed to mold-contaminated environments. Cellular and humoral immune responses and the presence of trichothecenes were evaluated in patients with mold-related health complaints. Patients underwent history, physical examination, skin prick/puncture tests with mold...

A series of chalcone-based macrocyclic ethers have been synthesized. These macrocyclic ethers contain polyether as well as extended conjugation to the benzene ring to function as fluorescent sensor for cations. The modeling studies show that the chalcone part of the receptors remains partially out of plane from the polyether part and the keto moiety of the receptors always directed outwardly in...

In the title thio-cyanate-coordinated aza-macrocyclic copper(II) complex, [Cu(NCS)(2)(C(24)H(38)N(6))], the Cu(II) atom is coordinated by the four secondary N atoms of the aza-macrocyclic ligand and by the two N atoms of the thio-cyanate ions in a tetra-gonally distorted octa-hedral geometry. The average equatorial Cu-N bond length is shorter than the average axial Cu-N bond length [2.010 (2) a...

Cell-penetrating peptides are widely used as molecular transporters for the internalization inside cells of various cargo, including proteins and nucleic acids. A special role is played by arginine-rich peptides and oligoarginines covalently linked or simply mixed with the cargo. Here we report cell-penetrating agents in which arginine units are clustered on a macrocyclic scaffold. Instead of u...

Schiff base condensation of benzil bis(hydrazone) with formaldehyde, acetone and benzaldehyde and its nickel(II) complexes were synthesised. Preparation of the free ligands was accomplished by refluxing benzil with hydrazine derivatives in 1:10 mole ratios in ethylene glycol. The spectral characterisation of hydrazone based 14-membered octaaza macrocyclic complexes of nickel(II) was undertaken....

The syntheses of seven macrocyclic analogues of the neuroprotective tripeptide glycyl-L-prolyl-L-glutamic acid (GPE) are described. Macrocycles 6 and 7 mimic the cis conformer of GPE whereas macrocycles 2-5, 8, and 9 mimic the trans conformer of GPE. The macrocyclic peptides of well-defined geometry were prepared via Grubbs ring closing metathesis of an appropriate diene precursor. In turn each...

A BODIPY-labeled macrocyclic heptaoxazole, L1BOD-7OTD, was developed as a fluorescent ligand for G-quadruplexes. The results of the study show that L1BOD-7OTD both selectively induces the formation of intramolecular G-quadruplexes from some G-quadruplex forming oligonucleotides (GFOs). In addition, the labelled macrocyclic heptaozaxole strongly binds to and stabilizes intramolecular G-quadruple...

Three novel complexes of Cu(II), Co(II) and Zn(II) using a macrocyclic ligand derived by the condensation of diethylphthalate and benzidine have been designed,synthesized and characterized by UV-Vis.,IR,Mass and Elemental analyses data in order to find out their antifungal activities. The stoichiometry of the complexes has been found to be 1: 1(Metal : Ligand). The analytical data indicate that...