Interplay between conformational flexibility, intermolecular H-bonding and 3d-metal cation extraction ability in a series of thiacalix[4]arene lower rim disubstituted Schiff base derivatives.

The rational design of organic ligands with the aim to control their binding abilities towards different metal ions can be considered as one of the key concepts in supramolecular coordination chemistry. Regarding the macrocyclic compounds of thiacalix[4]arene family, this can be achieved the targeted modulation of macrocyclic platform rigidity as well as the proper choice of appended binding sites. Four macrocyclic salen-type ligands based on lower rim disubstituted thiacalix[4]arene derivatives, adopted in a cone conformation, bearing highly coordinating iminophenolic or catecholic groups and two -CH- moieties as spacers but presenting different abilities to form H-bonds, were chosen to elucidate the interplay between the conformational flexibility of the macrocyclic ligands, propensity to participate in the intermolecular H-bonding and the extraction ability of 3d-metal cations.

(2-Hydroxy-3-Methoxybenzylidene)thiazolo[3,2-]pyrimidines: Synthesis, Self-Assembly in the Crystalline Phase and Cytotoxic Activity.

A series of new 2-hydroxy-3-methoxybenzylidenethiazolo[3,2-]pyrimidines with different aryl substituents at the 5 position are synthesized and characterized by H/ C NMR and IR-spectroscopy and mass-spectrometry, as well as single crystal X-ray diffraction (SCXRD). It was demonstrated that the type of hydrogen bonding can play a key role in the chiral discrimination of these compounds in the crystalline phase. The hydrogen bond of the O-H.

Synthesis, Self-Assembly in Crystalline Phase and Anti-Tumor Activity of 2-(2-/4-Hydroxybenzylidene)thiazolo[3,2-]pyrimidines.

A series of new thiazolo[3,2-]pyrimidines different by aryl substituents in 2 and 5 positions are synthesized and characterized in solution as well as in the crystalline phase using H and C NMR-, IR-spectroscopies, mass-spectrometry methods, and single crystal X-ray diffraction (SCXRD). The SCXRD study revealed the role of intermolecular H-bonding in the formation of supramolecular architectures (racemic monomers, centrosymmetric racematic dimers, or homochiral 1D chains) of obtained thiazolo[3,2-]pyrimidines derivatives depending on solvents (aprotic DMSO or protic EtOH) used upon the crystallization process. Moreover, the in vitro study of cytotoxicity toward different tumor cells showed their high or moderate efficiency with moderate cytotoxicity against normal liver cells which allows to consider the obtained thiazolo[3,2-]pyrimidine derivatives as promising candidates for application as antitumor agents.

Influence of 10-(6-plastoquinonyl) decyltriphenylphosphonium on free-radical homeostasis in the heart and blood serum of rats with streptozotocin-induced hyperglycemia.

Background: It is known that under conditions of tissue tolerance to insulin, observed during type 2 diabetes mellitus (DM2), there is an increased production of reactive oxygen species. Moreover, the free radicals can initiate lipid peroxidation (LPO) in lipoprotein particles. The concentration of LPO products can influence the state of insulin receptors, repressing their hormone connection activity, which is expressed as a reduction of the glucose consumption by cells.

Efficacy and safety of blonanserin transdermal patch in patients with schizophrenia: A 6-week randomized, double-blind, placebo-controlled, multicenter study.

Background: Blonanserin is a second-generation antipsychotic used for the treatment of schizophrenia. This study determined the efficacy, safety and pharmacokinetics of a blonanserin transdermal patch in patients with acutely exacerbated schizophrenia.

Methods: This double-blind, multicenter, phase 3 study consisted of a 1-week observation period during which patients were treated with two patches of placebo, followed by a 6-week double-blind period where patients were randomized (1:1:1) to receive once-daily blonanserin 40 mg, blonanserin 80 mg, or placebo patches.