10.1016/j.bmcl.2014.09.067
The study focuses on the design, synthesis, and evaluation of hydrophilic bisazole analogs as potential correctors for the most common cystic fibrosis (CF) mutation, the deletion of phenylalanine residue 508 in the CF transmembrane regulator conductance (CFTR) protein. The aim is to develop small molecules that can correct the misfolding of defective DF508-CFTR, which is retained in the endoplasmic reticulum and rapidly degraded, leading to impaired chloride transport and the associated symptoms of CF. The researchers synthesized and tested five more hydrophilic bisazole analogs of a previously identified bithiazole CF corrector, with the goal of identifying new CFTR correctors with less hydrophobicity and potentially increased hydrophilicity and stronger hydrogen bonding interactions within the DF508-CFTR binding site. The chemicals used in the study include various bisazole derivatives such as thiazole-tethered imidazolones, oxazoles, oxadiazoles, and thiadiazoles, which were designed to replace one of the two thiazole rings in the lead compound to explore different chemotypes and improve the drug's pharmacokinetic properties. The purpose of these chemicals was to assess their DF508-CFTR corrector activity and to understand the structure-activity relationships within this series of bisazoles.
10.1016/j.tet.2009.09.109
The research focuses on the development of a one-pot preparation method for 2,5-disubstituted and 2,4,5-trisubstituted oxazoles from alkyl aryl ketones using iodoarene-mediated reactions with Oxone and trifluoromethanesulfonic acid (TfOH) in various nitriles. The purpose of this study was to create a more efficient and less toxic method for synthesizing oxazoles, which are important heterocyclic units in biologically active natural products and medicinal chemistry. The researchers concluded that iodoarene acts as a catalyst in the reaction, allowing for the oxidative reactions to be carried out under metal-free conditions, and that Oxone is a more cost-effective oxidant compared to other reagents like m-chloroperbenzoic acid.
10.1016/j.poly.2011.08.012
The research focuses on the synthesis and coordination chemistry of specific phosphinoylmethyl-substituted oxazole and benzoxazole ligands with lanthanide ions. The study involves the development of ligands such as [(diphenylphosphinoyl)methyl]-4,5-dihydrooxazole (2) and [(diarylphosphinoyl)methyl]benzoxazoles with various aryl groups. These ligands were characterized using spectroscopic methods and single crystal X-ray diffraction. The coordination chemistry with Nd(NO3)3 and Yb(NO3)3 was examined, resulting in the formation of various complexes whose structures were determined. The ligands demonstrated both monodentate and bidentate coordination modes depending on the conditions, providing insights into their potential use in forming complexes with f-block metal ions.
10.3184/174751915X14192609116136
The research focuses on developing a novel copper-catalysed oxidative cyclisation method for synthesising trisubstituted oxazoles. Oxazoles are significant structures in numerous bioactive natural products and exhibit various biological activities. The study optimised the reaction conditions using ethyl acetoacetate and benzylamine as model substrates in the presence of a copper source in CH3CN at 60 °C under an O2 atmosphere, achieving a yield of 79%. The optimised conditions were then applied to synthesise various oxazole derivatives using different 1,3-dicarbonyl compounds and benzylamine derivatives. Key chemicals involved in the research include ethyl acetoacetate, benzylamine, copper catalysts such as [Cu(o-phen)2Cl]Cl, iodine, and various 1,3-dicarbonyl compounds and benzylamine derivatives used as substrates. The developed method is considered green as it avoids the use of hazardous materials and provides an efficient alternative for oxazole synthesis.
