synthesis and characterization of 6-(hydroxymethyl)-14, 16-dimethyl-13, 14, 16, 17-tetrahydro-6h-13, 17-epiminodibenzo [e, l] [1, 4] dioxacyclotridecin-15 (7h)-oneabstractnew 6-(hydroxymethyl)-14, 16-dimethyl-13, 14, 16, 17-tetrahydro-6h-13, 17-epiminodibenzo [e, l] [1, 4] dioxacyclotridecin-15 (7h)-one (2a) was synthesized in good yield by the petrenko–kritchenko reaction of 2, 2'-((3-hydroxyp...

The macrocyclic 5,5,7,12,12,14-hexamethyl-1,4,8,11-tetraazacyclotetradeca-7,14-dienium bromide salt (LBr) was synthesisedfor use in complexationreactions with various metal salts of copper, nickel, and zinc. Twelve complexes were synthesised; five of them were successfully obtained in a crystal form that was suitable for X-ray crystallographic analysis. All the complexes were analysedby microel...

A comprehensive analysis was done to evaluate the potential use of anti-parasitic macrocyclic lactones (including avermectins and milbemycins) for Buruli ulcer (BU) therapy. A panel containing nearly all macrocyclic lactones used in human or in veterinary medicine was analyzed for activity in vitro against clinical isolates of Mycobacterium ulcerans. Milbemycin oxime and selamectin were the mos...

A thermodynamic approach to peptide macrocyclization inspired by the cyclization of non-ribosomal peptide aldehydes is presented. The method provides access to structurally diverse macrocycles by exploiting the reactivity of transient macrocyclic peptide imines toward inter- and intramolecular nucleophiles. Reactions are performed in aqueous media, in the absence of side chain protecting groups...

Increasing the diversity of peptide cyclization methods is an effective way of accessing new types of macrocyclic chemotypes featuring a wide variety of ring sizes and topologies. Multicomponent reactions (MCRs) are processes capable of generating great levels of molecular diversity and complexity at low synthetic cost. In an attempt to further exploit MCRs in the field of cyclopeptides, we des...

Macrocycles are a structural class bearing great promise for future challenges in medicinal chemistry. Nevertheless, there are few flexible approaches for the rapid generation of structurally diverse macrocyclic compound collections. Here, an efficient method for the generation of novel macrocyclic peptide-based scaffolds is reported. The process, named here as "MacroEvoLution", is based on a c...

The photomagnetic properties of a new Fe(II) macrocyclic family [Fe(L(xyz)N5)(CN)2]·nH2O were investigated with respect to the T(LIESST) versus T(1/2) relationship. These compounds are diamagnetic below 400 K with T(LIESST) values above 100 K, which indicates that this family presents an unconventional LIESST effect that is much higher than the expected T0 = 180 K line for macrocyclic complexes.

The phenol-diamide compound, 5-(tert-butyl)-2-hydroxy-N1,N3-bis(2-hydroxyethyl)isophthalamide (), is water-soluble, non-cytotoxic, and capable of both, trapping ROS species and chelating Cu(ii) and Fe(iii) ions; these combined properties confer a protective effect against ROS induced cell death.