A class of 36 new 2-(6-phenylimidazo[2,-1-b][1,3,4]thiadiazol-2-yl)-1H-indoles was efficiently synthesized and evaluated for their anti-biofilm properties against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923, S. aureus ATCC 6538 and Staphylococcus epidermidis AT...

Imidazo[2,1-b][1,3,4]thiadiazole heterocycle was discovered during the 1950s. Since then, many newer derivatives are being developed and evaluated for their biological profiles. The derivatives of imidazo[2,1-b][1,3,4]thiadiazoles are widely explored for their biological potential viz. antimicro...

Racemic N-CBZ-3-fluoropyrrolidine-3-methanol (±)-1 was resolved by preparative chiral HPLC. The absolute configuration of the enantiomers of 1 was identified by vibrational circular dichroism and confirmed by chemical synthesis, which involved exchanging the CBZ protecting group of (−)-1 with B...

Methyl 2,3,4-tri-O-acetyl-d-glucopyranuronate reacts with phenols under Mitsunobu conditions to give β-phenylglucuronides. Improved yields are obtained with p-methyl and p-methoxyphenol by prior complexation to the chromium tricarbonyl residue, which serves to increase the acidity of the phenol.

In the present study, the silver nanoparticles were synthesized using a solution combustion method with urea as fuel. The prepared silver nanoparticles show an FCC crystalline structure with particle size of 59 nm. FESEM image shows the prepared silver is a rod like structure. The surface-enhanc...

Sulfonamides are the most famous agents, which have been utilized for preparation of effective antiproliferated agents. Therefore, this article describes the synthesis of new series of N-ethyl-N-methylbenzenesulfonamide derivatives having various biologically active moieties such as, thiazoles 3...

The stereoselective syntheses of thienyl and furyl analogues of ephedrine starting from (R)- and (S)-cyanohydrins, respectively, are described. Addition of methyl Grignard to the O-trimethylsilyl protected optically active cyanohydrins (R)- and (S)-3 and hydrogenation of the resulting imino inte...

The construction of different types of substituted arenes was demonstrated through the photocyclization of 2-(fur-3-yl)ethenylarenes using a 3-furyl group as an isopropenyl equivalent synthon in the photocyclization reaction. The furan portion of the photocyclization intermediate could be fragme...

Rapid Overlay of Chemical Structures (ROCS), which can rapidly identify potentially active compounds by shape comparison, is recognized as a powerful virtual screening tool. By ROCS, a class of novel Hsp90 inhibitors was identified. The calculated binding mode of the most potent hit 36 guided us...

A series of tetrahydropyridopyrimidine derivatives were synthesized and evaluated for neurotoxicity and peripheral analgesic activity followed by assessment of antiallodynic and antihyperalgesic potential in two peripheral neuropathic pain models, the chronic constriction injury (CCI) and partia...

Chemical optimization of the 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidine (THPP) scaffold was conducted with a focus on cellular potency while maintaining high selectivity against PI3K isoforms. Compound 11f was identified as a potent, highly selective and orally available PI3Kδ inhibitor. In addi...

Ether-free poly(p-phenylene)-based anion exchange membrane materials with outstanding vanadium ion blocking properties are reported. The synthesized ionomers with a rigid backbone structure show small dimensional variations despite the high ion exchange capacities. Among the synthesized membrane...

In this study, Cyphos IL 102 (trihexyl(tetradecyl)phosphonium bromide) diluted in toluene has been explored as an organic phase for the extraction, separation and recovery of V(V) from sulphate medium. The influence of different fundamental extraction variables namely acids and extractant concen...

Tensimetric and liquid ammonia extraction studies on the system VBr3NH3 show that the overall ammoniate VBr3.7NH3, formed at −36° is a mixture of VBr2NH2.5NH3 and NH4Br. The ammonobasic vanadium (III) bromide is soluble in liquid ammonia solutions of ammonium bromide so that VBr3 is largely s...

Evolution of bromine gas in the positive half cell of the Generation 2 (G2) vanadium bromide (V/Br) battery during charging is a concern which can be resolved by the use of bromine complexing agents. In this paper, for the first time, we report the effect of the addition of two quaternary ammoni...

The role and the importance of the sulfonate moiety in phenyl 4-(2-oxo-3-alkylimidazolidin-1-yl)benzenesulfonates (PAIB-SOs) were assessed using its bioisosteric sulfonamide equivalent leading to new cytochrome P450 1A1 (CYP1A1)-activated prodrugs designated as 4-(3-alkyl-2-oxoimidazolidin-1-yl)...

N,O-Aminals are synthesized through the N-iodosuccinimide-mediated regioselective 1,2-additions of alcohols to allenamides. These novel reactions proceed rapidly and exhibit broad substrate scope for a variety of allenamides. The reaction demonstrates that N-Iodosuccinimide is effective in activ...

Protein kinase A (PKA) is an important signal transduction target for drug development because it influences critical cellular processes implicated in neuropsychiatric illnesses such as major depressive disorder. The goal of the present study was to develop the first imaging agent for measuring ...

An efficient and highly regioselective synthesis of 2-amino-3-arylindoles via the BF3-promoted reaction of 3-diazoindolin-2-imines with aryl aldehydes is described. This reaction could be carried out under mild reaction conditions with a broad scope of substrates. Moreover, the operation is of p...

Widespread use of commercially available palladium precatalysts is limited by high costs and their synthetic challenges. In this report, series of synthetically affordable, phosphine-free ligands were examined as supports for palladium active centers. 2-(2-Aminoethylamino)ethanol, diethylenetria...