Eco-friendly, one-pot, solvent-free synthesis of biologically active 2-substituted benzimidazoles is presented and discussed herein. Novel N-Mannich bases are synthesized from benzimidazoles, secondary amines and formaldehyde, and their structures are confirmed by 1H nuclear magnetic resonance (...

A one-pot, three-component, microwave irradiated and conventional solution-phase synthesis of bioactive venlafaxine analogs such as 2,3-disubstituted-1,3-thiazolidin-4-ones 3a–j under mild conditions and their characterization are reported. The novel thiazolidin-4-ones, 3-(2-(1-hydroxycyclohexy...

A series of upper rim-functionalized calix[4]arene-based l-Proline derivatives have been synthesized and employed for the enantioselective aldol reactions between cyclic ketones and aromatic aldehydes in the presence of water. Good to excellent yields (up to 96%), enantioselectivities (up to 99%...

Maleimide groups were bound to the 3′-amino position of daunorubicin through a benzamide bond or to the 13-keto position through a benzoyl hydrazone or phenylacetyl hydrazone bond. The acid labile transferrin conjugates prepared with the latter two derivatives exhibited high activity in human m...

Ultrafine fluorescent fibers were prepared by electrospinning of a phenyleneethynylene oligomer mixed in DMF with a poly(styrene-co-maleimide) (PSM). The microscopic characterization by SEM reveals that the fibers are smooth and entangled one to the others forming a non-woven mat with an average...

In an effort to radiolabel antibodies, N-(m-[125I]iodophenyl)maleimide (m-[125I]IPM) was prepared by the demetallation of an N-[m-tri-(n-butyl)stannylphenyl]maleimide intermediate. The unlabeled intermediate was synthesized in ⩾ 75% yield using a palladium catalyzed reaction of hexabutylditin wi...

Inhibitory effect to endocannabinoid system-related human monoglyceride lipase (MGL) and selectivity toward fatty acid amid hydrolase of promising maleimide derived inhibitors were investigated by molecular docking and QSAR study. The essential roles of Ala61, Ser132 and His279 related hydrogen ...

A factor impeding the advancement of cell mediated therapy is the inability to track these cells in vivo by noninvasive techniques. It has been shown that cells express high levels of sulfhydryl groups. We sought to explore these groups to covalently label cells with radiolabeled maleimide deriv...

Acetaminophen overdose is the most common cause of acute liver injury (ALI) or acute liver failure in the United States. Its pathogenetic mechanisms are incompletely understood. Additional studies are warranted to identify new genetic risk factors for more mechanistic insights and new therapeuti...

We demonstrate a redox-sensitive nanofluidic diode whose ion rectification is modulated by the oxidation and reduction of chemical moieties incorporated on its surface. To achieve this goal, we have first synthesized the chemical compounds 1-(4-aminobutyl)-3-carbamoylpyridin-1-ium (Nic-BuNH2) an...

A series of dihalide M(II) mononuclear complexes in a cis configuration, Mn(HL1)2Cl2·CH3OH·H2O (1), Co(HL1)2Cl2·CH3OH·H2O (2), Ni(HL1)2Cl2·2H2O (3) and CoL2Cl2·0.5dmf (4) (HL1 – Schiff base ligand 4-N-(2′-pyridylimine)benzoic acid; L2 – pyridin-2-yl(3-(pyridin-2-yl)imidazo[1,5-a]pyridin...

Monoacylglycerol lipase (MAGL) is a major serine hydrolase that hydrolyses 2-arachidonoylglycerol (2-AG) into arachidonic acid (AA) and glycerol in the brain. Because 2-AG and AA are endogenous biologically active ligands in the brain, the inhibition of MAGL is an attractive therapeutic target f...

Syntheses for new potentially chelating ligands, 2,6-bis((1H-pyrazol-1-yl)methyl)pyridine 1-oxide (2), ((6-((1H-pyrazol-1-yl)methyl)pyridin-2-yl)methyl)diphenylphosphine oxide (4) and 2-((1H-pyrazol-1-yl)methyl)-6-((diphenylphosphoryl)methyl)pyridine 1-oxide (5), that are based upon pyridine or ...

The effective synthesis of pharmacologically oriented heterocyclic ensembles, [2-(1H-pyrazol-1-yl)thiazol-4-yl]furoxans, comprising furoxan moiety as NO-donor and pharmacophoric pyrazolylthiazole fragment is based on the condensation of (2-hydrazinylthiazol-4-yl)furoxan hydrobromides with linear...

The correct topogenesis of peroxisomal membrane proteins is a crucial step for the formation of functioning peroxisomes. Although this process has been widely studied, the exact mechanism with which it occurs has not yet been fully characterized. Nevertheless, it is generally accepted that perox...

Peroxisomes have the intrinsic ability to produce and scavenge hydrogen peroxide (H2O2), a diffusible second messenger that controls diverse cellular processes by modulating protein activity through cysteine oxidation. Current evidence indicates that H2O2, a molecule whose physicochemical proper...

We evaluated the effect of Ascaris lumbricoides on Giardia duodenalis infection and TH1/TH2 type immune mechanisms toward this parasite in 251 rural parasitized and 70 urban non-parasitized school children. The children were classified according to light (0–5000 eggs/g faeces) or moderate (>500...

This study examined the potential of Escherichia coli (E. coli) and Ascaris lumbricoides (A. lumbricoides) eggs inactivation in faecal matter coming from urine diverting dehydrating toilets (UDDT-F) by applying high concentrations of volatile fatty acids (VFAs) during anaerobic stabilization. Th...

The interleukin-1 binding B15R protein of Vaccinia virus and murine T1 are related extracellular glycoproteins with similarity to the extracellular domain of interleukin-1 receptors. In cells infected with a recombinant Vaccinia virus directing the overexpression of T1, production of the endogen...

Despite the effectiveness of classic treatments and available diagnostic tools, cancer continues to be a leading world health problem, with devastating cancer-related death rates. Advances in oncolytic virotherapy have shown promise as potentially effective treatment options in the fight against...