A stereoselective chemoenzymatic synthesis of Fmoc-protected (2S,3S)-2-hydroxy-3-amino acids 6 is described. After the formation of cyanohydrin 2 from 2-furaldehyde in the presence of R-oxynitrilase and subsequent protection, 3 was transformed into fully protected ethanolamines 5. Ozonolysis pro...

Reactions of the title meso forms, (1R,2S)-1,2-di(2-furyl)-1,2-di(3-guaiazulenyl)ethane (1) and (1R,2S)-1,2-di(3-guaiazulenyl)-1,2-di(2-thienyl)ethane (2), with a two molar amount of TCNE in benzene at 25 °C for 5 h (for 1) and 48 h (for 2) under oxygen give new compounds, 2,2,3,3-tetracyano-4-...

N-Formylmethamphetamine (FMA) and N-acetylmethamphetamine (AMA) are suspected to be trace by-products in methamphetamine (MA) produced from pseudoephedrine using the Nagai reaction. However, these amides are not rational by-products of the Nagai reaction.FMA is an intermediate in the synthesis o...

A novel and efficient iodine-catalyzed one-pot reaction of aromatic amines, acetophenones, and elemental sulfur for the synthesis of 2-aryl benzothiazoles is described. The process involves sequential C−S and C-N bond formation followed by C(CO)−C bond cleavage from readily accessible starting m...

Cis-3-hexen-1-yl acetate is a significant green note flavor compound and widely used in the food and cosmetic industry. In this research, a series of solid base KOH/γ-Al2O3 have been prepared and been utilized for the synthesis of cis-3-hexen-1-yl acetate via transesterification from cis-3-hexe...

Plants synthesize specialized metabolites which possess extremely important ecological functions including direct defense, indirect defense, and signaling. The optimal defense theory (ODT) proposes that defensive metabolites are preferentially allocated to the tissues with high fitness value or ...

Aspergillus oryzae, isolated from traditional Japanese food “Miso”, has efficiently catalyzed the direct esterification between acetic acid and cis-3-hexen-1-ol in organic solvent. The esterification between acids and alcohols having different chain lengths was initially investigated, observin...

The compound 1,8-diacetoxy-9,10-anthraquinone has been synthesised. Thin films coatings of this material have been prepared by thermal evaporation on glass substrates at different temperatures in vacuum. The experimental conditions have been optimised to obtain better crystallinity of the films....

The effects of members of a new class anticonvulsants, the tetronic acid derivatives, were studied in 3 in vitro models of epileptogenesis in rat hippocampal slices; the picrotoxin, the low magnesium and the low calcium model. The effects of AO33 (losigamone) and AO78 on stimulus-induced decreas...

The aim of this study was the isobolographic evaluation of interactions between two enantiomers of losigamone, AO-242 [(+)-5(R)-α(S)-5-(2-chlorophenylhydroxymethyl)-4-methoxy-2(5H)-furanone] and AO-294 [(-)-5(S)-α(R)-5-(2-chlorophenylhydroxymethyl)-4-methoxy-2(5H)-furanone], and valproate, car...

The aim of this study was the isobolographic evaluation of interactions between losigamone (LSG), valproate (VPA), carbamazepine (CBZ), phenytoin (PHT), and phenobarbital (PB) in the maximal electroshock (MES) test in mice. Electroconvulsions were produced by means of an alternating current (ear...

An assay based on a single-step liquid–liquid extraction from human plasma followed by high-performance liquid chromatography on a chiral column was developed for the measurement of enantiomers of a racemic new candidate antiepileptic drug. Excellent intra- and inter-assay accuracy and precisio...

Ion currents such as M-currents (IM), persistent sodium currents (INaP) and H-currents (Ih) have been observed in a variety of brain regions, including the hippocampal formation, where storage and retrieval of information are facilitated by oscillatory network activities. They have been suggeste...

Losigamone is an anticonvulsant both in vivo and in vitro. We here studied possible mechanisms for such effects with conventional intracellular recordings from pyramidal cells of area CA1 and entorhinal cortex in combined hippocampal-entorhinal cortex slices. Losigamone reversibly reduced the nu...

Losigamone (LSG) has shown anticonvulsant efficacy and low neurotoxicity in preclinical testing and has been tolerated in Phase I clinical trials. We report an open-label, add-on tolerability study of six ascending LSG dosage levels from 600 to 2,100 mg daily in patients receiving phenytoin (PHT...

Losigamone is a new antiepileptic drug with an unknown mechanism of action. Here we report on the effects of losigamone on the synaptic activity in a network of cultured rat hippocampal neurons. Losigamone dose dependently reduced the frequency of spontaneous synaptic events without affecting th...

The objective of the study was to investigate the efficacy and safety of two different dosages of Losigamone (LSG) in add-on treatment of partial seizures. In a multi-center, double-blind, randomized clinical trial, patients received one of three 12-week treatments: placebo, LSG 1200 mg/day, or ...

The tetronic acid derivative losigamone is a new anticonvulsant drug with a mechanism of action that was previously unknown. The drug decreases the frequency of spontaneous action potentials and suppresses repetitive firing of neurons. Here we tested the hypothesis that losigamone suppresses the...

In the search for developing a biomedicine based nanomaterial for therapeutic applications, here we described a new benign development of Photo-triggered Gold nanodots capped mesoporous silica nanoparticles [email protected] loaded with capsaicin (Cap) for photothermal therapy of cancer cells. E...

Capsaicin (CPS) and sulforaphane (SFN) have shown anti-carcinogenic, anti-inflammatory and antifibrogenic properties. The molecular mechanisms describing how these food compounds act remain unclear. This study was aimed at evaluating the molecular mechanisms of CPS and SFN on the hepatoprotectiv...