The pharmacologic activity profile of aletamine closely resembles that of the tricyclic antidepressants imipramine and amitriptyline. Effects shared are antagonism of RO4-1284-induced ptosis and depressed exploratory behavior, depression of spontaneous motor activity, prolongation of hexobarbita...

The electrochemical oxidation of mefexamide N-[2-(diethylamino)ethyl]-2-(4-methoxyphenoxy)acetamide was investigated using cyclic, linear scan and rotating disk voltammetry at glassy-carbon electrodes. The value of pKa (9.01) was determined by the potentiometric method. In cyclic voltammetry, in...

Thiourea derivatives (1–38) were synthesized and evaluated for their urease inhibition potential. The synthetic compounds showed a varying degree of in vitro urease inhibition with IC50 values 5.53 ± 0.02–91.50 ± 0.08 μM, most of which are superior to the standard thiourea (IC50 = 21.00 ± ...

Several novel 3-allyl-2-(substituted imino)-4-phenyl-3H-thiazole derivatives were synthesized by the reaction of allyl-thioureas and 2-bromoacetophenone. We also report the synthesis of bis-allyl-3H thiazoles using the reaction of various isothiocyanates and 1,3-phenylenediamine. The structures ...

Hydrogen sulfide (H2S) is a biologically important gaseous molecule that exhibits promising protective effects against a variety of pathological processes. For example, it was recognized as a blood pressure lowering agent. Aligned with the need for easily modifiable platforms for the H2S supply,...

Bisaromatic thioureas are widely used in e.g. asymmetric organocatalysis and considered to be robust compounds. Herein we show, in strong contrast to common notion, that thioureas dissociate to amines and isothiocyanates in a base catalyzed reaction under mild conditions. This ‘unclicking’ pro...

1-(4-Haloisoquinolin-1-yl)ureas are generated efficiently via a tandem reaction of 2-alkynylbenzaldoxime, carbodiimide, with halide in water. The process involves the generation of halonium ion in situ by employment of NaI/oxone or NaBr/oxone as the promoters. This green process proceeds smoothl...

At this circumstance for the first time, a facile and convenient method for heteroaryl ureas has been developed via a two-step process involving in situ C–OH activation followed by palladium catalyzed C–N coupling of heteroarenols with ureas, which show excellent functional group tolerance and...

New benzofuranylthiazole derivatives containing the aryl–urea moiety were synthesized and evaluated in vitro as dual acetylcholinesterase (AChE)-butyrylcholinesterase (BuChE) inhibitors. In addition, the cupric reducing antioxidant capacities (CUPRAC) and ABTS cation radical scavenging abilitie...

A facile and versatile method for the synthesis of unsymmetrical ureas from readily available reagents is reported. In the first step trifluoroethylchloroformate is reacted with a stoichiometric amount of a primary amine to give an intermediate trifluoroethyl carbamate. The addition of a second ...

The increasing interest on new drug discovery is constantly up to date as drugs do not increase survival adequately against increasing cancer cases worldwide. Based on the reported anticancer activity of coumarin, chalcone and urea derivatives, the present investigation dealt with the design and...

Novel primaquine semicarbazides 7a–l and ureas 9a–g with modified benzhydryl, trityl, phenyl or hydroxyalkyl substituents were prepared and evaluated for cytostatic and antioxidative activities. Two synthetic approaches for preparation of the title semicarbazides were applied, both having cert...

An efficient synthetic procedure has been achieved for selective synthesis of 1,5-disubstituted tetrazoles and diaryl ureas from secondary amides in situ in the presence of NaN3 and POCl3 as solvent, both by conventional and microwave methods. The reaction conditions were optimized to yield sele...

The synthesis of bicyclic ureas and sulfamides via palladium-catalyzed alkene carboamination reactions between aryl/alkenyl halides/triflates and alkenes bearing pendant cyclic sulfamides and ureas is described. The substrates for these reactions are generated in 3–5 steps from commercially ava...

High-quality single crystals of 1,3-bis(4-methoxyphenyl)prop-2-en-1-one (BMP) of size 20 mm×16 mm×5 mm have been grown by the slow evaporation of an acetone solution at 28 °C and characterized by elemental analysis, thermo-gravimetric analysis/differential thermal analysis (TGA/DTA), Fourier ...

An organic nonlinear optical (NLO) material 1,3-bis(4-methoxyphenyl)prop-2-en-1-one (BMP) single crystal has been successfully grown by vertical Bridgman stockbarger technique (VBT) using single wall ampoule. The grown crystal was subjected to single-crystal X-ray diffraction analysis (SXRD) to ...

Solid-phase extraction (SPE) (reversed-phase and mixed-mode) and nylon membranes were investigated as solid matrices for obtaining fluorescence signals from adsorbed triamterene (TA). Although a significant emission was found in all investigated surfaces, solid-phase extraction systems yielded t...

A recombinant β-glucosidase from Caldicellulosiruptor saccharolyticus DSM 8903 with a specific activity of 13 U/mg was purified by heat treatment and His-Trap affinity chromatography and identified as a single 54 kDa band on SDS-PAGE. The molecular mass of the native enzyme was 108 kDa as a dim...

A β-galactosidase exhibiting maximal activity at pH 1.0 was purified from Teratosphaeria acidotherma AIU BGA-1. The enzyme had a molecular mass of 180 kDa and consisted of two heterosubunits of 120 kDa and 66 kDa. The N-terminal amino acid sequence of the large subunit was found to be SPNLQDIVT...

A series of (Z)-1-(1,3-diphenyl-1H-pyrazol-4-yl)-3-(phenylamino)prop-2-en-1-one derivatives were synthesized and characterized by 1H and 13C NMR, ESI-MS and HRMS. All the synthesized compounds were evaluated for their anticancer activity against HT-29, PC-3, A549 and U87MG human tumor cell lines...