We investigated the effects of a novel bradycardic agent, bertosamil (3-isobutyl-7-isopropyl-9,9-pentamethylene-3,7-diazabicyclo[3.3.1]nonane sesquihydrogenfumarate), on the sinus rate and atrial contractile force and the left ventricular contractile force in isolated, blood-perfused dog hearts ...

A series of ethyl 6-bromo-5-hydroxy-1H-indole-3-carboxylates, 8a–11v, were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities in 2.2.15 cells. The selective indexes of inhibition on replication of HBV DNA of compounds 11s (>8.7) and 11t (10.8), which were introduced hal...

ObjectiveHSV-2 infection has increased significantly in recent years, which is closely associated with cervical cancer and HIV infection. The lack of success in vaccine development and the emergence of drug resistance to commonly used drugs emphasize the urgent need for alternative antivirals ag...

Influenza virus infections are the main contagious respiratory disease with high levels of morbidity and mortality worldwide. Antiviral drugs are indispensable for the prophylaxis and treatment of influenza and other respiratory viral infections. In this study, the Arbidol hydrochloride (ARB), w...

The purpose of this study was to cover the bitter taste of arbidol hydrochloride (ARB) and develop dry suspension with combination of solid dispersion and flavors. Taste masking was successfully done by solid dispersion using octadecanol as the carrier by fusion method. Suspending agents, carrie...

The synthesis, in vitro ligand binding study and in vivo Elevated Plus Maze test (EPM) of a series of pyrazolo[4,3-c]quinolin-3-ones (PQs) are reported. Multistep synthesis of PQs started from anilines and diethyl 2-(ethoxymethylene)malonate to give the quinolin-4-one nucleus, via the Gould-Jaco...

Phenyl substituted imidazoles exhibit versatile biological activity. 1-(R-phenyl)-1H-imidazoles with different functional groups R provide a convenient suitcase of molecules with tunable physicochemical properties adjustable for many practical applications. In this work, the absolute vapor press...

Two new mixed ligand complexes [Ni(en)2(mot)2] (1) and [Cu(en)2(mot)2] (2) derived from potassium N′-(4-methoxy-benzoyl) dithiocarbazate [K+(H2L)−] containing en as the coligand have been synthesized. [K+(H2L)−] undergoes cyclization in the presence of ethylenediamine and is converted to 5-(4-m...

Three new mixed ligand complexes [Cd(en)2(4-mpot)2] (1) [Ni(2-pytone)2(en)2] (2) and [Ni(2-mpot)2(en)2] (3) {4-mpot = 5-(4-methoxy-phenyl)-1,3,4-oxadiazole-2-thione, 2-pytone = 5-(2-pyridyl)-1,3,4-oxadiazole-2-thione, 2-mpot = 5-(2-methoxy-phenyl)-1,3,4-oxadiazole-2-thione} have been prepared co...

Escherichia coli growing under anaerobic conditions produces H2 and CO2 by the enzymatic cleavage of formate catalyzed by formate hydrogenlyase (FHL) consisting of a molybdoenzyme formate dehydrogenase H (fdhF), hydrogenase 3 (hyc), and intermediate electron carriers (hyc). Transcription of both...

The metabolism of N,N-dimethylformamide in the Sprague—Dawley rat has been reinvestigated using NMR spectroscopy of urine. In particular, through the use of N,N-dimethylformamide-d7 (DMF-d7) and 2H-NMR spectroscopy, the principal metabolites of this compound have been confirmed in a direct mann...

β-Galactosidase from Aspergillus oryzae, α-galactosidase from Aspergillus niger, β-mannosidase from Helix pomatia and β-glucosidase from almond were used to synthesise different glycosides by reverse hydrolysis: GlcβO(CH2)6OH 1 was obtained in 61% yield, β-D-Glc-O(CH2)3CH-CH2 2 in 50% yiel...

The regio- and stereoselective glycosylation at the 6-position in 2,3,4,6-unprotected hexopyranosides has been investigated with dibutyltin oxide as the directing agent. Perbenzylated hexopyranosyl bromides were employed as the donors and the glycosylations were promoted by tetrabutylammonium br...

Inhibition of TLR4 signaling is an important therapeutic strategy for intervention in the etiology of several pro-inflammatory diseases. There has been intensive research in recent years aiming to explore this strategy, and identify small molecule inhibitors of the TLR4 pathway. However, the rec...

Perfluoroalkanesulfonamide organocatalyst 7 efficiently promotes asymmetric Michael additions of malonates to enones in cyclohexane or water to produce the corresponding addition products with excellent yields and with up to 99% ee.

In the presence of catalytic amount of Cu(OTf)2/trisoxazoline, an enantioselective Friedel–Crafts reaction of N-methyl pyrrole with alkylidene malonates has been developed and up to 66% ee is achieved.

An efficient catalytic protocol for Pd-catalyzed decarboxylative cross-coupling of potassium malonate monoesters and derivatives with aryl bromides and chlorides are described. Because of its broad applicability, this new catalytic system provides an alternative method for the preparation of div...

Deprotonations of dimethyl (4-nitrophenyl)malonate (C-acid) by 7-methyl-1,5,7-triazabicyclo[4.4.0]dec-5-ene (MTBD), 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD) and 1,8-bis(dimethylamino)naphthalene (DMAN) in acetonitrile were studied by kinetic as well as FTIR and 1H NMR spectroscopic methods. In ...

The addition of carboxylic acids enhances the rate and selectivity of alkene oxidations catalyzed by [(bpmen)Fe(OTf)2] (bpmen = N,N′-dimethyl-N,N′-bis(2-pyridylmethyl)-1,2-diaminoethane). The syntheses and characterizations of four derivatives of this iron complex with varying substitutions on...

Spectrum deficiency in red component of YAG: Ce3+ phosphor is hopeful to be made up by small amount of Si4+-N3− replacing Al3+-O2− for high quality lighting, while the important indicators of emission efficiency and thermal quenching properties dramatically decrease in this approach. Thus micro-...