Search

2,3-dihydro[1,5] benzothiazepines and diazepines can be prepared by condensation of o-aminothiophenol or o-phenylenediamines with a variety of 3-chlorothieno-or benzothienopropanones.

The synthesis of β-lactams was carried out by N-arylpropionamide cyclisation in a mixture of N,N-dimethylformamide and anhydrous sodium carbonate under nitrogen atmosphere with 50 to 90% yield.

The first medical cure of Acanthamoeba keratitis was obtained by use of propamidine isethionate. Since then, it has been the basic drug recommended for use in treatment. Because some Acanthamoeba strains have been reported to be resistant to propamidine and propamidine was found to be only weakly cysticidal, superior homologs such as butamidine, pentamidine, hexamidine, heptamidine, octamidine, and nonamidine were tested for their amoebicidal effects on two Acanthamoeba strains isolated from patients with keratitis. Trophozoicidal and cysticidal efficiencies were found to be increased from propamidine to nonamidine; i.e., when the alkyl chain connecting the two benzene rings in their molecular structures was elongated, in comparison with propamidine, hexamidine and octamidine were the most amoebicidal molecules. As a result of these data, a kinetic study carried out on propamidine, hexamidine, and octamidine demonstrated that the amoebicidal effects resulted from two events: the diffusion of molecules through the plasma membrane or the double wall of trophozoites or cysts, respectively, and the lethal effects of molecules on amoebic protoplasm. The diffusion kinetics were increased when the alkyl chain was elongated, i.e., with an increase in the lipophilic properties of molecules. In contrast, the lethal effect kinetics were found to be unchanged by this elongation, indicating that they originated from the cationic surface-active properties induced by the protonated amidine groups attached to each benzene ring, which themselves remained unchanged from one molecule to the other. These results strongly advocate the immediate replacement of propamidine by hexamidine in the medical treatment of Acanthamoeba keratitis; in France, 0.1% hexamidine eyedrops are available (Desomedine). The results also advocate clinical investigations on the efficiency and toxicity of octamidine, which appears to be the most amoebicidal diamidine in vitro.

The applicative potentiality of the nanotechnologies emerges more and more in all fields of science, technology, and medicine. In this context, magnetic nanoparticles have been recently proposed as promising nanomaterials to eliminate, through minimally invasive treatments, small tumours. This work deals with the design and realization of electrospun hybrid membranes of Polycaprolactone (PCL) incorporating magnetic nanoparticles modified with the acid citric-based ligand. The nature of the ligand allows very effective compatibility between nanoparticles and hosting fibers, as deducible by the nanoparticles distribution along the fibers. Dimension and functionalization of the nanoparticles, together with the optimization of the electrospinning parameters allow obtaining highly homogeneous distribution in the diameter of the nanocharged fibers, which ranges between 500 nm and 3 μm. The anticancer activity of the optimized electrospun hybrid membranes has been analyzed toward two different melanoma cell lines: the low metastatic A375 and the high metastatic A2058, using the MTT assay. The formulated membrane exhibited a dose-dependent reduction toward both melanoma cells viability, without a decrease of activity compared to the unfunctionalized Fe3O4nanoparticles. Promising results have been obtained also considering the antitumor activity of the hybrid Membranes toward uterine HeLa cells. Magnetic properties and structural and morphological characteristics of the functional membranes highlight very promising applications for tuning/enhancing the nanodelivery of drugs and chemotherapy assisted by electroporation technique.

Carbazoles are aromatic heterocyclic compounds derived from the fusion of a benzene ring with an indole nucleus in 2,3 position. Today, many carbazole derivatives are widely studied as anticancer, anti-fungal, antioxidants, photoconductor, anti-bacterial, antimalarials, anti-Alzheimer, anti-tuberculosis, anti-HIV agents and for the treatment of obesity. Some of them, differently substituted on carbazole nucleus, have been synthetized and their biological activity have been evaluated. The purpose of this work is the study of new species obtained binding, a series of carbazole derivatives in which the carbazolic nitrogen has been functionalized with different alkyl-thiol chains, with gold nanoparticles, synthesized in organic solvent. The formation of self-assembled monolayers of these ligands is obtained on the spherical surface of gold nanoparticles, with a stabilizing effect against aggregation. These systems might present a double innovative function, matching an antineoplastic activity typical of carbazoles, with the photothermal effects of gold nanoparticles.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.