ANATOMICO-SURGICAL FOUNDATIONS OF DUODENOJEJUNAL CHANGE AT THE CHRONIC DUODENAL OBSTRUCTION

Anatomic and clinical research of duodenojejunal change in norm, and at the chronic duodenal obstruction, of functional character was realized. Peculiarities of motor-evacuation disorders + were revealed with help of X-ray method and peripheral computed, electrogastroenterography. Sizes, variants of forms of duodenojejunal change in norm, and in pathology were determined with, use of endoscopic method

Novel potent pyridoxine-based inhibitors of AChE and BChE, structural analogs of pyridostigmine, with improved in vivo safety profile

© 2016 Elsevier LtdWe report a novel class of carbamate-type ChE inhibitors, structural analogs of pyridostigmine. A small library of congeneric pyridoxine-based compounds was designed, synthesized and evaluated for AChE and BChE enzymes inhibition in vitro. The most active compounds have potent enzyme inhibiting activity with IC50 values in the range of 0.46–2.1 μM (for AChE) and 0.59–8.1 μM (for BChE), with moderate selectivity for AChE comparable with that of pyridostigmine and neostigmine. Acute toxicity studies using mice models demonstrated excellent safety profile of the obtained compounds with LD50 in the range of 22–326 mg/kg, while pyridostigmine and neostigmine are much more toxic (LD50 3.3 and 0.51 mg/kg, respectively). The obtained results pave the way to design of novel potent and safe cholinesterase inhibitors for symptomatic treatment of neuromuscular disorders

Ion assisted deposition of titanium chromium nitride

Chromium titanium nitride films with different content of Cr and Ti were deposited on a silicon substrate by ion beam assisted deposition and characterised by Rutherford Backscattering Spectroscopy, X-ray Diffraction, X-ray Photoelectron Spectroscopy (XPS), Cross-sectional Transmission Electron Microscopy and nanoindentation testing. All of the samples except for the pure Cr2N coating have a structure similar to the fcc form of TiN (111). XPS data showed that the films contained a small amount of oxygen. The dependence of hardness on film composition was observed. Maximum hardness at about 30 GPa was for coatings containing 15 at.% Ti and 35 at.% Cr. The high hardness in the ternary compound is thought to be attributed to high energy of dislocation propagation. It has been shown that chromium nitride formed in the absence of atomic nitrogen always grows as Cr2N. The addition of atomic nitrogen using an ion assisting beam promotes growth of CrN. The presence of a relatively low amount of Ti in the Ti–Cr–N film was seen to promote a significant increase in the number of Cr–N bonds. Preferential sputtering of nitrogen from the film during Ar ion cleaning for XPS analysis shows that composition analysis by XPS can be unreliable and should be done with great care

Novel potent pyridoxine-based inhibitors of AChE and BChE, structural analogs of pyridostigmine, with improved in vivo safety profile

© 2016 Elsevier LtdWe report a novel class of carbamate-type ChE inhibitors, structural analogs of pyridostigmine. A small library of congeneric pyridoxine-based compounds was designed, synthesized and evaluated for AChE and BChE enzymes inhibition in vitro. The most active compounds have potent enzyme inhibiting activity with IC50 values in the range of 0.46–2.1 μM (for AChE) and 0.59–8.1 μM (for BChE), with moderate selectivity for AChE comparable with that of pyridostigmine and neostigmine. Acute toxicity studies using mice models demonstrated excellent safety profile of the obtained compounds with LD50 in the range of 22–326 mg/kg, while pyridostigmine and neostigmine are much more toxic (LD50 3.3 and 0.51 mg/kg, respectively). The obtained results pave the way to design of novel potent and safe cholinesterase inhibitors for symptomatic treatment of neuromuscular disorders

Novel potent pyridoxine-based inhibitors of AChE and BChE, structural analogs of pyridostigmine, with improved in vivo safety profile

© 2016 Elsevier LtdWe report a novel class of carbamate-type ChE inhibitors, structural analogs of pyridostigmine. A small library of congeneric pyridoxine-based compounds was designed, synthesized and evaluated for AChE and BChE enzymes inhibition in vitro. The most active compounds have potent enzyme inhibiting activity with IC50 values in the range of 0.46–2.1 μM (for AChE) and 0.59–8.1 μM (for BChE), with moderate selectivity for AChE comparable with that of pyridostigmine and neostigmine. Acute toxicity studies using mice models demonstrated excellent safety profile of the obtained compounds with LD50 in the range of 22–326 mg/kg, while pyridostigmine and neostigmine are much more toxic (LD50 3.3 and 0.51 mg/kg, respectively). The obtained results pave the way to design of novel potent and safe cholinesterase inhibitors for symptomatic treatment of neuromuscular disorders