The Botryosphaeriaceae are a family of trunk disease fungi that cause dieback and death of various plant hosts. This work sought to characterize fatty acid derivatives in a highly virulent member of this family, Lasiodiplodia theobromae. Nuclear magnetic resonance and gas chromatography-mass spe...

A novel series of symmetrically substituted 3,3-dibenzyl-4-hydroxy-3,4-dihydro-1H-quinolin-2-ones was synthesized and tested as antimicrobials. The minimum inhibitory concentration (MIC) values of the most active heterocycles were slightly higher than those exhibited by levofloxacin, employed as...

To clarify the mechanism of the species difference in the metabolism of bisoprolol enantiomers, in vitro metabolic studies were performed using dog liver microsomes and human cytochrome P450 (CYP) isoforms. The O-deisopropylation of bisoprolol enantiomers showed biphasic kinetics in dog liver mi...

(±)-1-[4-(2-Isopropoxyethoxymethyl)-phenoxy]-3-isopropylamino-2-propanol (bisoprolol) is a potent, clinically used β1-adrenergic agent. (R)-(+) and (S)-(−) enantiomers of bisoprolol were labelled with carbon-11 (t1/2=20.4 min) as putative tracers for the non-invasive assessment of the β1-adre...

□ The plasma concentrations and urinary excretions of bisoprolol enantiomers in four Japanese male healthy volunteers after a single oral administration of 20 mg of racemic bisoprolol were evaluated. The AUCǴ∞ and elimination half-life of (S)-(–)-bisoprolol were slightly larger than those of ...

The stereoselective pharmacokinetics of bisoprolol, a highly β1-selective adrenoceptor blocking agent, was studied in dogs. After intravenous and oral administration of the racemate, there was a difference in the plasma concentration between S(−)- and R(+)-bisoprolol. The area under the curve (...

Background/aimPyrimidine is found as a core structure in a large variety of compounds that exhibit important biological activity. Specifically, 2,4,5,6-tetrasubstituted dihydropyrimidines have shown potent antimycobacterial activity. The use of combinatorial approaches toward the synthesis of dr...

Model studies show that displacement of fluorine, rather than chlorine, occurs upon reaction of 3,5-dichloro-2,4,6-trifluoropyridine with sodium methoxide and phenoxide. Subsequent hydro-dechlorination can be achieved by reaction with lithium aluminium hydride whereas reaction of sodium in iso-p...

The normal mode frequencies and corresponding vibrational assignments of 3,5-dichloro-1,2,4-trithia-3,5-diborolane (B2S3Cl2) are examined theoretically using the Gaussian98 set of quantum chemistry codes. All normal modes were successfully assigned to one of six types of motion predicted by a gr...

The solid phase mid FTIR and FT-Raman spectra of 3,5-dibromopyridine (3,5-DBP) and 3,5-dichloro-2,4,6-trifluoropyridine (3,5-DCTFP) have been recorded in the regions 4000–400 cm−1 and 3500–100 cm−1, respectively. The spectra were interpreted with the help of normal coordinate analysis (NCA) fo...

Three new diorganotin(IV) complexes of the formulae [Me2Sn(cdet)] (2), [Bu2Sn(cdet)] (3) and [Ph2Sn(cdet)] (4) have been synthesized by the reaction of 3,5-dichloro-2-hydroxybenzaldehyde-N(4)-ethylthiosemicarbazone [H2cdet, (1)] and appropriate diorganotin(IV) chloride in the presence of KOH in ...

The reactivity of 3,5-dichloro-4H-1,2,6-thiadiazine 4,4-ketals towards nucleophilic substitution or palladium-catalyzed C–C coupling at the C-3/5 positions led to seven new 3,5-disubstituted 4H-1,2,6-thiadiazine ethylene glycol 4,4-ketals and seven 3,5-disubstituted 4H-1,2,6-thiadiazine catecho...

An efficient base-promoted 3-alkylation of 3,5-dichloro-2(1H)-pyrazinones with various malonate esters is described. The method constitutes a simple example of a C–C bond forming process at the 3-position of the pyrazinone core allowing to attain 3-substituted pyrazinones in good to high yields...

3,5-Diaryl-2,4,6-trifluoropyridines and 5-aryl-3-chloro-2,4,6-trifluoropyridines were prepared through Suzuki–Miyaura reactions of 3,5-dichloro-2,4,6-trifluoropyridine with arylboronic acids in high yields.

Background and purposeProtein modification by small ubiquitin-like modifier (SUMO) plays a critical role in the pathogenesis of heart diseases. The present study was designed to determine whether ginkgolic acid (GA) as a SUMO-1 inhibitor exerts an inhibitory effect on cardiac fibrosis induced by...

Ginkgolic acids (GAs) in natural product Ginkgo biloba L. are the pharmacological active but also toxic components. Two compounds, GA (C15:1) and GA (C17:1) are the most abundant GAs. In this study, several in vitro and in vivo models were applied to investigate transport mechanism of GAs. A rap...

A highly sensitive method using ultra-high-pressure liquid chromatography coupled with linear ion trap-Orbitrap tandem mass spectrometry (UHPLC–LTQ–Orbitrap–MS) has been developed and validated for the simultaneous identification and quantification of ginkgolic acids and semi-quantification o...

Infection by enterohemorrhagic Escherichia coli O157:H7 (EHEC) is a worldwide problem, and there is no effective therapy. Biofilm formation is closely related to EHEC infection and is also a mechanism of antimicrobial resistance. Antibiofilm screening of 560 purified phytochemicals against EHEC ...

An efficient method for the preparative separation and isolation of ginkgolic acids (GAs) from the sarcotesta of Ginkgo biloba L was developed by combining pH-zone-refining counter-current chromatography (PZRCCC) with inner-recycling mode. Two grams of GAs extract were separated by PZRCCC using ...

Ginkgolic acids and urushiols are natural alkylphenols known for their mutagenic, carcinogenic and genotoxic potential. However, the mechanism of toxicity of these compounds has not been thoroughly elucidated so far. Considering that the SIRT inhibitory potential of anacardic acids has been hypo...