Human aldose reductase (AKR1B1, AR) is a key enzyme of the polyol pathway, catalyzing the reduction of glucose to sorbitol at high glucose concentrations, as those found in diabetic condition. Indeed, AKR1B1 overexpression is related to diabetes secondary complications and, in some cases, with c...

In this paper, we have described the conventional and microwave methods for the synthesis of 1-[2-(2-chloro-6-methyl(3-quinolyl))-5-(4-nitrophenyl)(1,3,4-oxadiazolin-3-yl)]-3-(aryl)prop-2-en-1-ones (4a–l). Through this method, we have observed a decrease in reaction time and a better yield than...

A new series of 2-phenol-4-chlorophenyl-6-aryl pyridines were designed, synthesized, and evaluated for topoisomerase (topo) I and II inhibitory activities as well as cytotoxic activity against four different human cancer cell lines such as HCT15, T47D, DU145, and Hela. Most of the tested compoun...

Malondianilide (I) derived from p-chloroaniline was cyclized to 6-chloro-4-hydroxyquinoline-2(1H)-one (II) in moderately good yield using polyphosphoric acid as catalyst. This compound was then coupled with some diazotized aromatic amines to give the corresponding azo disperse dyes 1–12. A syst...

6-Chloro-2-Aryl-1H-imidazo[4,5-b]pyridine derivatives 1–26 were synthesized and characterized by various spectroscopic techniques. All these derivatives were evaluated for their antiglycation, antioxidant and β-glucuronidase potential followed their docking studies. In antiglycation assay, com...

5-(4-Chlorophenyl amino)-2-mercapto-1,3,4-thiadiazole (I) was refluxed with formaldehyde and ammonium chloride in ethanol yielding the Mannich base 5-(4-chloro phenyl amino)-3-aminomethyl-2-mercapto-1,3,4-thiadiazole (II). Esterification with 4-chloro-(2,6-dinitro phenoxy)-ethyl acetate (III) un...

A series of novel 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives were synthesized and evaluated for anti-hepatitis B virus (anti-HBV) activities in vitro to explore their structure–activity relationships (SARs). Most of the synthesized compounds possessed potent a...

Twenty-four 2-(4-oxo-2-thioxothiazolidin-3-yl)acetic acid (rhodanine-3-acetic acid)-based amides, esters and 5-arylalkylidene derivatives were synthesized, characterized and evaluated as potential antimicrobial agents against a panel of bacteria, mycobacteria and fungi. All of the derivatives we...

Crystal structures of five ortho-, meta-, and para-substituted benzoic acid derivatives, 2-fluoro-4-hydroxymethyl benzoic acid (1), 4-chloro-3 nitrobenzoic acid (2), 5-bromo-2-methyl benzoic acid (3), 4-bromo-2 nitrobenzoic acid (4) and 4-chloro-2-iodobenzoic acid (5) have been determined using ...

The acrylic monomer, 3,5-dimethylphenyl methacrylate was synthesized by reacting 3,5-dimethylphenol dissolved in ethyl methyl ketone (EMK) with methacryloyl chloride in the presence of triethylamine. The homopolymer and various copolymers with glycidyl methacrylate were synthesized using free ra...

Two heteroleptic iridium complexes, (dmppy)2Ir(tmd) and (dmppy)2Ir(acac), which consist of phenylpyridin (ppy) as main ligand with dimethyl substituents on both the phenyl ring and the pyridine ring, and heptanedione (tmd) and acetyl acetonate (acac) as ancillary ligands were synthesized and cha...

Using the alternating-current electrochemical technique, the novel π-complex [CuI(m-dmphast)NH2SO3] (1), based on the 5-(allylthio)-1-(3,5-dimethylphenyl)-1H-tetrazole (m-dmphast) ligand, was obtained and it was studied by single crystal X-ray diffraction as well as IR and UV–Vis spectroscopy....

Fluorescent phenenthrimidazole derivatives have been synthesized and characterized by 1H, 13C NMR and mass spectral analyses. Synthesized compounds have been. The solvent effect on the absorption and fluorescence bands has been analyzed and supplement by computational studies. Phenenthrimidazole...

A series of eight biologically active N, N′-disubstituted thiocarbamide compounds (1–8) have been prepared from thiophene-2-carbonyl isothiocyanate and various substituted aromatic primary amines (2,4-dichlorophenyl aniline, 4-chloro-3-nitrophenyl aniline, 4-methoxycarbonylphenyl aniline, 3-me...

Fifteen new thiobarbituric acids have been prepared by the Knoevenagel condensation of appropriate aldehydes with 1-(2,3, 2,5, 2,6 dichlorophenyl)-3-morpholinophenyl thiobarbituric acids. Five compounds of this series were found to be biphasic in nature whereas some compounds showed appreciable ...

A series of palladium (II) complexes (1–8) with N-(acyl)-N′,N′-(disubstituted) thioureas and phosphine ligands were synthesized and characterized by FT-IR, multinuclear (1H, 13C & 31P) NMR spectroscopy and elemental analysis. The crystal structures of the Pd(II) complexes (1) & (5) of the typ...

The organophosphorus (OP) compound O-hexyl-O-2,5-dichlorophenyl phosphoramidate (H-DCP) is hydrolysed in the plasma, liver and brain of hens and rats. We study in hen plasma the effect of tissue and substrate concentrations and of pH on the hydrolysing activity of H-DCP. The data on each tissue ...

O-Hexyl O-2,5-dichlorophenyl phosphoramidate (HDCP) is a chiral organophosphorus compound that undergoes enzymatic hydrolysis in the rat and hen. Studies of the stereospecificity of its biodegradation are necessary to establish HDCP toxicity. To this effect, methods have been developed for the a...

Neuropathy target esterase (NTE) is a membrane protein present in various tissues whose physiological function has been recently suggested to be the maintenance of phosphatidylcholine homeostasis. Inhibition and further modification of NTE by certain organophosphorus compounds (OPs) were related...

2,6-Dichlorophenyl methylsulphone and a number of structurally related chemicals are CYP-activated toxicants in the olfactory mucosa in mice and rats. This toxicity involves both the olfactory neuroepithelium and its subepithelial nerves. In addition, 2,6-dichlorophenyl methylsulphone induces gl...