Methamphetamine (MA) and amphetamine (AM) are widely abused drugs. These compounds contain a chiral center, and their enantiomers exhibit different pharmacologic, pharmacokinetic, and metabolic properties due to differences in binding affinities to their receptor sites. Until now, there was a la...

Inhaled terbutaline is commercially available β2-agonist which consists of equivalent amount of R- and S-enantiomer. In this study, we aimed to investigate the effects of single enantiomers of terbutaline and its racemate in an ovalbumin (OVA)-induced mouse model of asthma via. seven days inhal...

The N-methyl-d-aspartate receptor (NMDAR) antagonist (R,S)-ketamine has robust antidepressant effects in depressed patients although it has detrimental side effects such as psychotomimetic and dissociative symptoms. (R,S)-Ketamine is known to cause the expression of heat shock protein HSP-70 (a ...

We introduce the notions of strongly Lipschitz (p,r,s)-nuclear operators and strongly Lipschitz (p,r,s)-integral operators. We develop a theory of strongly Lipschitz (p,r,s)-nuclear operators and strongly Lipschitz (p,r,s)-integral operators which closely parallels the theory for linear operator...

Although glucocorticoids (GCs) are widely used as anti-inflammatory drugs, they are often accompanied by adverse effects, which are mainly due to the transactivation of glucocorticoid receptor (GR) target genes. In order to screen novel plant-derived GR ligands (phytocorticoids) capable of separ...

(R, R)-Rhizoferrin and (R, S, R)-staphyloferrin A are carboxylate-type siderophores. Their streamlined synthesis has been accomplished starting from (R)-citric acid. Key-step of these syntheses is a chemo-enzymatic ester hydrolysis. (S, S)-rhizoferrin was accessible by a multistep synthesis star...

Efficient synthesis of benzofuroquinolizine ketone 1 was accomplished in four steps from ethyl 3-benzofuranacetate. The O-analogue of the Pictet-Spengler cyclization was used to form the benzofuroquinolizine ring structure as a key step.

L-657, 743 (MK-912), a highly potent and selective α2-adrenoceptor antagonist was tritiated to a high specific activity and its binding characteristics to brain tissue were determined. The specific binding of [3H]L-657, 743 to rat cerebrocortex was saturable, reversible, and dependent on tissue...

We used MK-912, a potent new selective α2-adrenergic receptor antagonist that is active orally, to study the effect of short-term, selective α2-blockade on fasting plasma glucose (FPG) and pancreatic islet function in non-insulin-dependent diabetes (NIDDM). Ten asymptomatic patients with NIDDM...

ABSTRACT. In vitro studies showed that MK-912 ((2S, 12bS)1’,3’-dimethylspiro(1,3,4,5’,6,6’,7,12b-octahydro-2H-benzo[b]furo[2,3-a]quinolizine)-2,4’-pyrimidin-2’-one) is a potent α2-adrenergic receptor antagonist with high affinity (Ki = 0.42, 0.26 and 0.03 nM to α2A, α2B and α2C, respec...

How and why the chemical stability of amorphous solid is different from crystalline solid is an important problem. In this study, this problem is addressed by evaluation of the photodegradation of both crystalline and amorphous MK‐912 (an α‐2 adrenoceptor antagonist) according to the photosta...

The discovery of new methods for stereoselective glycoside synthesis and convergent oligosaccharide assembly has been critical for the area of glycosciences. At the heart of this account is the discussion of the approaches for stereoselective synthesis of glycosides of 2-amino-2-deoxysugars that...

The reaction of 2-methyl-2-((1-phenylethyl)amino)propanenitrile with different γ-halocarbonyl compounds is investigated. The influence of different parameters such as the nature of the substrate and solvent, is discussed. The reaction is considered as a convenient route to 2-cyanopyrrolidines i...

2-Pyrone derivatives were prepared in a one step procedure from readily available (chlorocarbonyl)phenyl ketene and 1,3-diketones such as 2,4-pentanedione, 1,3-diphenyl-1,3-propanedione, 1-phenyl-1,3-butanedione, 1,3-cyclohexanedione, 5,5-dimethyl-1,3-cyclohexanedione, 1,3-dimethyl-pyrimidine-2,...

Good nucleophilicity of the ring nitrogen in chiral (2R,1′R)-2-acyl-(1′-phenylethyl)aziridines initiated the reaction with various acid chlorides to form the corresponding acylaziridinium ion intermediates whose rings were opened by the chloride anion to yield the β-amino-α-chlorocarbonyl co...

This Letter describes the amination of 3-bromoisoxazoles by a nucleophilic aromatic substitution reaction. We have found 3-bromoisoxazoles to be inert to substitution under thermal conditions, however, the employment of phosphazene bases under microwave irradiation facilitates the amination proc...

An efficient transformation of 2-aryl-1,1-dibromocyclopropanes under the action of sulfur trioxide activated nitrosyl chloride has been developed, providing a series of arylated 5-bromoisoxazoles with good yields. It is noteworthy that under the reported conditions the nitrosation–heterocycliza...

A new series of diphenyl piperazine derivatives containing the phenyl substituted aminopropanol moiety, which were modified at sites between the diphenyl and piperazine moieties, was prepared and evaluated for dopamine transporter binding affinity with [3H]GBR12935 in rat striatal membranes. The...

The migration of plastic components or additives from packaging to food can produce a risk for human health, in fact many of these plasticizers and additives are “Endocrine Distruptors”, such as phthalates (PAEs), alkylphenols (APs), 2,2-bis(4-hydroxyphenyl)propane (bisphenol A or BPA) and di(...

A series of new 3-(1H-benzimidazol-2-yl)quinolin-2(1H)-one derivatives (5a1−5d6) were designed and synthesized as antitumor agents. In vitro antitumor assay results showed that some compounds exhibited moderate to high inhibitory activity against HepG2, SK-OV-3, NCI-H460 and BEL-7404 tumor cell ...