Bovine mastitis is the most significant economic drain on the worldwide dairy industry. Concerns regarding poor cure rates, emergence of bacterial resistance, and residues in milk necessitate development of alternative therapeutic approaches to antibiotics for treatment of mastitis. A variety of...

The electrochemical activation of C-X bonds requires very negative electrode potentials. Lowering the overpotentials and increasing the catalytic activity requires intensive electrocatalytic research. A profound understanding of the reaction mechanism and the influence of the electrocatalyst all...

Synthesis, crystal structure, Fourier transform infrared spectroscopy (FT-IR) and quantum mechanical studies of the 2-(4-bromobenzyl)-5-ethylsulphonyl-1,3-benzoxazole (C16H14NO3SBr) have been reported. The molecular structure obtained from X-ray single-crystal analysis of the investigated compou...

The reactivity of 1-(2-bromobenzyl)-4-halopyrazoles in inter- and intra-molecular Pd-catalysed direct arylation was investigated. Conditions allowing the intermolecular C5-arylations of both 1-(2-bromobenzyl)-4-chloropyrazoles and 1-(2-bromobenzyl)-4-bromopyrazoles, without cleavage of the pyraz...

The electrocatalytic activity of 10 cathode materials (Ag, Au, Cu, Glassy carbon (GC), Ni, Mg, Mn, Pb, Pt and Ti) was examined for the intramolecular cyclisation reaction of allyl 2-bromobenzyl ether to 2-methyl benzopyran. The influence of the cathode materials on the electrocatalytic activity ...

1-(Het)aryl-3-bromoprop-2-ynones react with 2-(2-furyl)pyrrole in the Al2O3 or K2CO3 dispersion (room temperature, 1 h) to afford the cross-coupling products either at the furan or pyrrole rings. Furan and 2-methylfuran with 3-bromo-1-phenylprop-2-ynone under the same conditions give the Diels–...

The hepatitis C virus (HCV) NS5B polymerase is an attractive target for the development of novel and selective inhibitors of HCV replication. In this paper, the design, synthesis, and preliminary SAR studies of novel inhibitors of HCV NS5B polymerase based on the structure of tegobuvir have been...

In this study, we synthesized and evaluated several amino 4-hydroxy-2(1H)-quinolone (4HQ) derivatives as new PET radioligand candidates for the glycine site of the NMDA receptors. Among these ligands, we discovered that 7-chloro-4-hydroxy-3-{3-(4-methylaminobenzyl) phenyl}-2-(1H)-quinolone (12) ...

The reaction between p-aminophenols 1 and various ketene acetals 2 in the presence of hypervalent iodine is described. The results show that 2- and 3-substituted 5-sulfonamidobenzofurans 3 are obtained in moderate to good yields from p-aminophenols and ketene acetals.

Geometric parameters, vibrational frequencies, conformer energy difference, and barriers to internal rotation for the cyclopropyl methyl ketone (CPMK, c-С3H5C(O)CH3) molecule in the ground electronic state were obtained by performing MP2, MP4(SDQ), CCSD, and CCSD(T) calculations and VFPA. Ab in...

Herein we describe an unprecedented formation of a cyclopropane ring through the conversion of a methyl group that was not functionalized for the purpose. In a one-step reaction, 7-deacetoxy-7α-hydroxygedunin (4) afforded two new gedunin derivatives, namely 7-deacetoxy-13,14,18-cyclopropyl-7α,...

Because of the rapid increase in deaths due to Staphylococcus aureus (S. aureus) infection, significant resources have been invested over the past decade in new treatments. Successful therapy requires amalgam of therapies to delineate the pathogen while providing protection to the host cell. Wit...

This study reports a facile and controllable synthetic method for the preparation of both 1,3- and 1,5-isomers of 4-(3(5)-aryl-3(5)-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamides, as well as a new series of 4-(3-aryl-5-hydroxy-5-(trifluoromethyl)-4,5-dihydropyrazol-1-yl)benzenesulfonamide...

An asymmetric deprotonation reaction allows for short syntheses of the lactones (5S, 6S)- Aeginetolide (1) and (5S)-Dihydroactinidiolide (2).

New oxovanadium(IV) pentane-2,4-dionate complexes decorated with long alkyl tails have been prepared and characterized by the spectroscopic methods and the X-ray crystallography. The increased solubility in non-polar organic solvents enabled to investigate the catalytic activity of the title com...

Melanin-concentrating hormone (MCH), which is a neuropeptide expressed in the hypothalamus of the brain, is involved in regulating feeding behavior and energy homeostasis via the MCH1 receptor in rodents. It is widely considered that MCH1 receptor antagonists are worthy of development for medica...

Accumulating evidence suggests that fibroblast growth factor receptor 1 (FGFR1) is an attractive target in gastric cancer therapy. Based on our previous discovery of two non-ATP competitive FGFR1 inhibitors, A114 and A117, we designed and screened a series of compounds with the framework of bisa...

A new generation of water soluble tetrazolium salts have recently become available and in this study we compared a colorimetric assay developed using one of these salts, 2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2, 4-disulfophenyl)-2H-tetrazolium, monosodium salt (WST-8), with a previousl...

Poly(2-methoxy-5-(2-(4-nitrophenyl)ethenyl)-1,4-phenylenevinylene) (PMNEPV) and a series of copolymers (poly(MNEPV-co-PV)) containing varying amounts of 1,4-phenylenevinylene (PV) units have been synthesized via soluble precursor polyelectrolytes. These polymers possess a unique structural featu...

Hartree-Fock (HF) and density functional theory (DFT) calculations have been carried out on the molecular structure of (E)-2-methoxy-4-[2-(4-nitrophenyl)ethenyl]-phenol (MNEP) which has interesting non-linear optical properties. This compound is also known as 4-methoxy-3-hydroxynitrostilbene in ...