Guinea-pig vasa deferentia were incubated with a 2-halogenoalkylamine (14C-SY28) either alone or after exposure to the alpha receptor blocking agent, phentolamine. A quantitative evaluation was made of the distribution of the covalently bound 14C-SY28 both in lipid and lipid-free phases, and the...

In this work, we further investigated a previously introduced class of cholinesterase inhibitors. The removal of the carbamic function from the lead compound xanthostigmine led to a reversible cholinesterase inhibitors 3. Some new 3-[ω-(benzylmethylamino)alkoxy]xanthen-9-one analogs were design...

A simple, efficient, and novel method has been developed for the synthesis of hexahydroxanthene-9-N-arylamine derivatives through a one-pot reaction of cyclohexanone and morpholine with salicylaldehyde imines in the presence of indium(III) chloride as a catalyst. 1-(4-Morpholino)-cyclohexene ena...

The aim of this study was evaluating the principle feasibility of biotechnological synthesis of drug metabolites using heterologously expressed human cytochrome P450 (CYP) enzymes. Human CYP2D6 expressed in fission yeast (Schizosaccharomyces pombe) strain CAD58 was used as model enzyme and the d...

Tranexamic acid (4-aminomethyl-cyclohexanecarboxylic acid) was reacted with sulfonyl chlorides to produce structurally related four sulfonamide derivatives using simple and environmental friendly method to check out their three-dimensional behavior and van der Walls interactions. The molecules w...

Owing to the biological importance of cyclic sulfonamides (sultams), herein we report a new, facile and cost-effective method for the synthesis of sultams that makes use of a reaction between dansyl amide and easily accessible benzaldehydes under mildly acidic conditions. All compounds were obta...

KMnO4-mediated oxidative CN bond cleavage of tertiary amines producing secondary amine was introduced, which was trapped by electrophiles (acyl chloride and sulfonyl chloride) to form amides and sulfonamides. The reaction could take place at mild condition, tolerating a wide range of function gr...

The detection of anions has attracted considerable interest because of their importance in various physiological processes. In this study, two sulfonamide and urea-based compounds (1a and 1b) were successfully developed and their spectroscopic and anion recognition properties were fully investig...

Herein, we report that acridine intermediates 5 were obtained from the reduction of nitro acridine derivatives 4, which were synthesized via condensation of dimedone, p-nitrobenzaldehyde with 4-amino-N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)benzamide, respectively. Then acridine sulfonamide/carboxam...

This study deals with the synthesis of benzophenone sulfonamides hybrids (1–31) and screening against urease enzyme in vitro. Studies showed that several synthetic compounds were found to have good urease enzyme inhibitory activity. Compounds 1 (N′-((4′-hydroxyphenyl)(phenyl)methylene)-4′′-...

The synthesis of hyaluronic acid oligosaccharides on polyethylene glycol (PEG) using an acylsulfonamide linker has been explored. Hyaluronic acid is a challenging synthetic target that usually involves the condensation of highly disarmed glucuronic acid building blocks. Amine-ended PEG monomethy...

A fluorometric method for determining guanisoquin in plasma, urine, and tissues, based upon the coupling of guanisoquin with ninhydrin in alkaline solution to form a highly fluorescent product, is described. Limited studies of the excretion and distribution in the rat and the dog indicated that ...

2-(Naphthalen-2-yl)benzo[d]thiazole meso fused dipyrromethene boron difluoride dyes are synthesised and their linear and non-linear optical properties are studied. The third order nonlinear susceptibility (χ3) value obtained from the Z-scan experiment is 11.21 × 10−13 and 13.30 × 10−13 esu. T...

Metalloprotease PT121Y114S, an effective catalyst for Z-aspartame synthesis under the substrate (Z-Asp:l-Phe-OMe) molar ratio of 1:5, was obtained previously. Herein, a computational strategy combining molecular dynamics simulation of the enzyme-substrate complex with binding free energy (ΔG) c...

The pentapeptide Z-(L)-Ala-(L)-Phe-Gly-(L)-Phe-Gly-OMe was obtained by reacting the activated dipeptide derivative Z-(L)-Ala-(L)-Phe-OPcp with the amino peptide derivative TFA·H-Gly-(L)-Phe-Gly-OMe at 100–105°C under reduced pressure (10−2-10-−3 Torr) without using solvents. The product obtai...

The aim of the present study was to investigate the effects of 5-bromo-2-hydroxy-4-methyl-benzaldehyde (BHMB) on inflammatory responses to lipopolysaccharide (LPS) in RAW 264.7 cells and the associated mechanism of action. BHMB concentration-dependently suppressed protein and mRNA expressions of...

Employing kinetic Monte Carlo, we simulated the radical chain propagation of the pyrolysis of phenethyl phenyl ether (PPE), which serves as a model compound for the β-O-4 linkage in lignin. The input rate constants were obtained with transition state theory based on density functional calculati...

In order to understand the mechanism of lignin pyrolysis, the pyrolysis of phenethyl phenyl ether (PPE) as dimeric lignin model compound was investigated by density functional theory methods at B3LYP/6-31G(d) level. Ten possible pyrolytic pathways were proposed including two concerted reactions ...

In this work, a partial oxidation treatment process in critical water was developed for high-efficiency dechlorination of waste polyvinyl chloride and the recovery of high value-added chemical feedstock. The partial oxidation treatment of waste polyvinyl chloride was performed at the temperature...

Trimethyl borate (TB) is used as an electrolyte additive to improve cyclic stability and rate capability of a layered cathode, LiNi1/3Co1/3Mn1/3O2 (LNCM), under 4.5 V (vs. Li/Li+). Charge/discharge tests demonstrate that the cyclic stability and rate capability of LNCM can be improved significan...