A simple and efficient method was developed for the synthesis of 1,4-thiazin-2-one O-(tert-butyl) oximes and benzo[b][1,4]thiazin-2-one O-(tert-butyl) oximes from N-tert-butoxy acyl imidoyl bromides and 2-aminothiols in the presence of K2CO3/SiO2. Twenty five novel compounds were readily synthes...

New carboxyl-containing o-aminophenols and phenoxazines were synthesized by condensation of 3,5-di-(tert.-butyl)-quinone with p-aminobenzoic and anthranilic acids. Oxidative transformations of the o-aminophenols and intermediate o-iminoquinones occur with the formation of the ESR detected phenox...

A facile synthesis of a wide variety of tert-butyl ethers and tert-butyl ester derivatives under mild conditions is described. Alcohols etherified with tert-butyl methyl ether as tert-butyl source and solvent, in the presence of sulfuric acid. Many amino acid tert-butyl esters have been synthesi...

2H-Pyran-2-ones are widely present in nature and found as either isolated or in fused form. Depending on the fusion of benzene ring, pyran can give coumarins, isocoumarins, dibenzopyrans etc. This class of molecules exhibit excellent biological activity and photophysical properties. Apart from t...

The minimum inhibitory concentrations (MICs) of tosufloxacin and other fluoroquinolone antimicrobials for Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella (Branhamella) catarrhalis, isolated, between January 2003 and July 2004, from patients suspected of having respiratory or otor...

We compared the antibacterial effects and the emergence of resistance to tosufloxacin or levofloxacin for Streptococcus pneumoniae by simulating the serum concentration according to the Japanese clinical regimens using an in vitro pharmacokinetic-pharmacodynamic model. For quinolone-susceptible ...

Quantum chemical calculations are performed over some boron complexes with tosufloxacin. Boron complex with fluorine atoms are optimized at HF/6-31+G(d), B3LYP/6-31+G(d) and M062X/6-31+G(d) level and the best level is determined by comparison of experimental and calculated results. The other com...

The interaction between tosufloxacin (TELX) and bovine lactoferrin (BLF) in aqueous solution was analyzed by fluorescence spectroscopy and absorbance spectra. The binding parameters and energy-transfer efficiency parameters were determined and the mechanism of interaction was discussed. The effe...

Macrolide-resistant Mycoplasma pneumoniae (MRMP) has emerged and is increasing worldwide. In a 2011 outbreak of MRMP infections in Japan, symptoms failed to improve in many patients who initially received macrolides; the therapeutic agent was then changed to minocycline (MIN), doxycycline (DOX) ...

BackgroundThe use of non-β-lactam agents has increased in Japan due to the prevalence of β-lactam-resistant pathogens. This study aimed to clarify the recent trend of antimicrobial susceptibility and molecular epidemiological features in Haemophilus influenzae.

This review presents a systematic survey of the literature (through the end of 2014) for de novo syntheses of 3-pyrrolin-2-ones from acyclic precursors or via transformation of other cyclic systems such as pyrroles, pyrrolidinone, and maleimides. One-component intramolecular cyclization approach...

Some 3-acetyl-2-substituted phenyl-5-(3,4,5-trimethoxyphenyl)-2,3-dihydro-1,3,4-oxadiazole derivatives were synthesized by cyclization reaction of N′-substituted benzylidene-3,4,5-trimethoxybenzohydrazide in acetic anhydride. Their structures were verified by elemental analysis, IR, 1H NMR, and...

A series of 3,4-disubstituted-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazoles and some novel 5,6-dihydro-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles bearing 3,4,5-trimethoxyphenyl moiety were synthesized and screened for their anticancer activity. The preliminary bioassay results indicated that comp...

A newly developed benzoylpiperidine drug that increases the size of fast, excitatory synaptic responses was examined for its effects on the kinetic properties of α-amino-3-hydroxy-5-methyl-4-isoxalepropionic acid-type glutamate receptors. When long pulses of glutamate were applied to excised hi...

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...

The discovery and synthesis of a series of 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A2A receptor antagonists from a small-molecule combinatorial library using a high-throughput radioligand-binding assay is described. Antagonists were further characterized in the A2A binding assay and ...

A series of 2-(5-nitro-2-furyl) and 2-(5-nitro-2-thienyl)-5-substituted-1,3,4-thiadiazoles (5a–d and 6a–j) were synthesized and evaluated against Leishmania major promastigotes using 3H-thymidine incorporation. Most of the compounds showed activity better than the reference drug sodium stibogl...

The recyclization of (2-aminophenyl)bis(5-tert-butyl-2-furyl)methane derivatives has been studied. It was shown that the acid-catalyzed recyclization of N-tosylamides leads to the formation of 2-(3-oxoalkyl)-3-(2-furyl)indoles. In contrast, under the same reaction conditions, acetamides are tran...

The conformations of E-2-phenyl-3(2′-furyl)propenoic acid and its methyl ester were investigated by NMR spectroscopy. Applying various solvents (methanol, chloroform and dimethyl sulfoxide) the possible conformers in solutions were studied by two-dimensional NOESY measurements. Irrespective to ...

A new, efficient, and simple process has been established for the synthesis of (3,5-diaryl-2-furyl)(aryl)acetonitriles by the reaction of various 2,4,6-triarylpyrylium perchlorates with sodium cyanide.