BackgroundSepsis is a common diagnosis in critical care with inpatient mortality rates up to 50%. Sepsis care is organized around source control, antibiotics, and supportive care. Drug disposition is deranged by changes in volume of distribution and regional blood flow, as well as multiple organ...

− (±)-5-Me-8-OH-DPAT 4 was synthesized by a new synthetic pathway recently described by us. The (+)- and (−)-enantiomers 4 were prepared from the primary amine 8 by crystallisation of the (+)- and (−)-mandelic acid salts. The enantiomers reacted with propyl iodide and were demethylated by 48% H...

An analogue of tetrodotoxin (TTX), 11-oxoTTX, was semi-purified from the red-spotted newt, Notophthalmus viridescens, and identified by ESI-MS and 1H NMR spectra. The levels of TTX, 11-oxoTTX and 6-epiTTX in early stage of development (efts) of this newt were investigated by a post-column fluore...

A novel tetrodotoxin analog was isolated from the puffer Arothron nigropunctatus and identified as 11-oxotetrodotoxin hydrate on the basis of NMR and chemical transformation studies.

IntroductionIguratimod (T-614) has been confirmed as a highly efficacious and safe novel disease-modifying anti-rheumatic drug (DMARD) for rheumatoid arthritis therapy in China and Japan due to its potent anti-inflammation effect. Here, we investigate the effects of Iguratimod on osteoclast diff...

Inflammatory bowel disease (IBD) is an autoimmune disease with an abnormal and persistent immune response. Iguratimod, a novel anti-rheumatic drug, exhibits anti-inflammatory effects and regulates immune response. The role of iguratimod in intestinal mucosal inflammation and immunity has not bee...

The structural requirements of retro-thiorphan, N-[1R,S-benzyl-2-mercaptoethyl]malonamic acid 2, analogs for the inhibition of endothelin converting enzyme (ECE) were investigated. Although based on a single amino acid residue, N-[1R-(1H-indol-3-ylmethyl)-2-mercaptoethyl]-2-phenylacetamide 28 wa...

The degradation of the enkephalinase inhibitor thiorphan was studied. Liquid chromatography UV and electrochemical detections and several techniques of spectrometry showed that the degradation was oxidative and generates diastereoisomers of the corresponding disulfide. The degradation kinetics o...

The molecular characterization of antithrombin Barcelona-2 is reported. The abnormal antithrombin was isolated from plasma by chromatography on heparin-Sepharose at pH 6.0, and ion exchange on DEAE-Sephadex at pH 8.6 and 6.0. The tryptic peptides were mapped by reverse-phase HPLC and amino acid ...

Raman (3400–100 cm−1) and infrared (4000–200 cm−1) spectra of 5-(methylthio)-1,3,4-thiadiazole-2(3H)-thione (C3H4N2S3; MTT) were measured in the solid state, and the 1H/13C NMR spectra were obtained in DMSO-d6. Initially, twelve structures were proposed as a result of thiol–thione tautomerism...

3-Sulfonyl and 3-aroylindoles have attracted special attention because of their interesting biological activities, particularly for the development of antiviral and anticancer compounds. Based on the importance of the trifluoromethyl group in biological active molecules, we have developed a synt...

Organic-inorganic hybrid aluminosilicate compounds KCS-3 and KCS-4 were successfully synthesized by low-temperature hydrothermal reaction of mother gels composed of organically-bridged silane, fumed alumina, alkali metal hydroxide and water. Two bridged organosilanes i.e. 4,4′-bis(triethoxysily...

New tetranuclear Cu(II) complex [Cu4(L)4]·MeCN (1) with 2,6-di(5-trifluoromethyl-1H-pyrazol-3-yl)pyridine (H2L) was synthesized. It has been shown that treatment of 1 with selected aza-ligands (pyridine, 2,2′- and 4,4′-bipyridyl, 2,3,5,6-tetra-(pyridine-2-yl)pyrazine, 2,2′;6′,2″-terpyridin...

Convenient methods for regioselective syntheses of Methotrexate peptidic conjugates are described. Solid phase synthesis for derivatives of Methotrexate containing an amide bond has been applied and showed higher efficiency than liquid phase synthesis. Synthetic pathways for regioselective prepa...

The chloro(ligand-C,N)triphenylphosphinepalladium(II) complexes with cyclopalladated N,N-dialkylbenzylamines (alkyl = methyl, ethyl and n-propyl), azobenzene, 8-methylquinoline, dimethylaminomethylferrocene and 2-benzylpyridine undergo lithium chloride-induced solvolysis in acetic acid solvent u...

A new series of quinoxalinones 6/7-trifluoromethyl or nitro- and 6,7-difluoro substituted bearing various side-chains (alkyl, halogenoalkyl, benzyl and phenyl groups) at C-3 of the ring system was synthesized and submitted to preliminary in vitro evaluation for antibacterial, antifungal, antimyc...

Pilicides are a class of compounds that attenuate virulence in Gram negative bacteria by blocking the chaperone/usher pathway in Escherichia coli. It has also been shown that compounds derived from the peptidomimetic scaffold that the pilicides are based on can prevent both Aβ aggregation and c...

In this work, the vibrational characteristics of 4-(trifluoromethyl) benzylbromide (TFMBB) have been investigated and both the experimental and theoretical vibrational data indicate the presence of functional groups in the title molecule. The density functional theoretical (DFT) computations wer...

Photoaffinity cross-linking enables the analysis of interactions between DNA and proteins even under denaturing conditions. We present a photoaffinity electrophoretic mobility shift assay (EMSA) in which two heterogeneous techniques―photoaffinity cross-linking using DNA bearing 3-trifluoromethy...

A new polydentate Schiff base ligand and its metal complexes were synthesized and characterized by elemental analyses, IR, 1H NMR, electronic, ESR and mass spectra, conductivity and magnetic susceptibility measurements as well as thermal analyses. The free ligand was synthesized by condensation ...