A series of novel carboxamide compounds 19a-19j, 20a-20j and 22a-22d containing piperazine and arylsulfonyl moieties have been synthesized. The bioassay results showed that some compounds exhibited favorable herbicidal activities against dicotyledonous plants and many of them possessed excellent...

The synthesis of proline analogues bearing a fluorine-containing substituent at the fifth position of the pyrrolidine ring, racemic trans- and cis-5-fluoromethyl prolines, was performed. The key step of the synthesis is a transformation of the CH2OH-group into the CH2F-one using morpholinosulfur...

(5,10,15,20-Tetrakis(4-(4-carboxyphenycarbonoimidoyl)phenyl)porphyrinato) chloro gallium(III) (complex 1) was conjugated to platinum nanoparticles (PtNPs) (represented as 1-PtNPs). The resulting conjugate showed 18 nm red shift in the Soret band when compared to 1 alone. Complex 1 and 1-PtNPs sh...

Some triazinone derivatives are designed and synthesized as potential antitumor agents. Triazinone derivatives 4c, 5e and 7c show potent anticancer activity over MCF-7 breast cancer cells higher than podophyllotoxin (podo) by approximate 6-fold. DNA flow cytometry analysis for the compounds 3c, ...

A library of 16 4-substituted 2-(1H-pyrrolo[3,2-c]pyridin-2-yl)propan-2-ols 17–32 has been synthesized for use in biological testing against Trypanosoma cruzi, the protozoan parasite that causes Chagas disease. The 4-substituted 2-(1H-pyrrolo[3,2-c]pyridin-2-yl)propan-2-ols 17–32 were subjecte...

The Peterson reaction between a series of 2-substituted 1-azabicyclo[2.2.2]octan-3-ones and 3-methyl-5-trimethylsilanylmethyl isoxazole (1) was explored. (Z)-Stereoselectivity was obtained with all 2-substituents, ranging from 65:35 for benzyl to 95:5 for phenylsulphanyl. Different bases were in...

ω-Aminoacyl and -alkyl derivatives of 4-(4-methylpiperazin-1-yl)bicyclo[2.2.2]octan-2-amines and of 5-(4-methylpiperazin-1-yl)-2-azabicyclo[3.2.2]nonanes were prepared and their activities were examined in vitro against the multiresistant K1 strain of Plasmodium falciparum and against Trypanoso...

A series of 3-(pyrazol-3-yl)-1-azabicyclo[2.2.2]octane derivatives C (Fig. 1Download high-res image (43KB)Download full-size imageFigure 1.

Loss of telomeres stability is a hallmark of cancer cells. Exposed telomeres are prone to aberrant end-joining reactions leading to chromosomal fusions and translocations. Human telomeres contain repeated TTAGGG elements, in which the 3′ exposed strand may adopt a G-quadruplex (G4) structure. T...

Sphingolipid derivatives cause diverse effects towards the regulation of intracellular free Ca2+ concentrations ([Ca2+]i) in a multitude of nonexcitable cells. In the present investigation, the effect of C-8 ceramide-1-(2-cyanoethyl) phosphate (C1CP) on store-operated Ca2+ (SOC) entry was invest...

Accurate and reliable methods are presented for the determination of enantiomeric excess values of glycidol (2,3-epoxy-1-propanol), glycidyl esters, solketal [2,2-dimethyl-4-(hydroxymethyl)-1,3-dioxolane], homologous 1,3-dioxolane alcohols and substituted primary propanols in biological samples....

Five novel lanthanide complexes [Ln2(2-ClQL)6(phen)2(H2O)2]·2H2O (Ln = Pr(1), Sm(2), Eu(3), Ho(4), Er(5)); 2-ClQL: 2-chloroquinoline-4-carboxylate; phen: 1,10-phenanthroline; were synthesized by conventional solution method at room temperature and characterized via elemental analysis, powder x-...

We conducted an experimental and quantum chemical investigation of the electronic properties and vibrational mode couplings of a structure analogous to a paracetamol (acetaminophen): 2-Bromo-N-(2-hydroxy-5-methylphenyl)-2-methylpropanamide. The spectroscopic and electronic properties were carrie...

BackgroundMice with functional ablation of the neurokinin-1 receptor gene (NK1R−/−) display behavioural abnormalities which resemble the hyperactivity, inattention and impulsivity seen in Attention Deficit Hyperactivity Disorder (ADHD). Here, we investigated whether the established ADHD treatmen...

We aimed to investigate whether microRNA-let-7d (miRNA-let-7d) and miRNA-107 may serve as diagnostic and therapeutic biomarkers of attention deficit hyperactivity disorder (ADHD). The relative expression level of miRNA-let-7d and miRNA-107 in patients with ADHD and in a healthy control group was...

To investigate the putative rewarding effects of atomoxetine, a non-stimulant medication for Attention-deficit/hyperactivity disorder (ADHD), we conducted conditioned place preference (CPP) tests in an animal model of ADHD, the spontaneously hypertensive rat (SHR). The effects of drug pre-exposu...

The impact of treatment with the noradrenaline (NA) re-uptake inhibitor atomoxetine and the α2-adrenoceptor (AR) antagonist idazoxan in an animal model of Parkinson’s disease (PD) was assessed. Concurrent systemic treatment with atomoxetine and idazoxan, a combination which serves to enhance t...

ObjectiveThe primary aim of this study was to assess the efficacy of atomoxetine in improving ADHD and ODD symptoms in paediatric patients with ADHD and comorbid oppositional defiant disorder (ODD), non-responders to previous psychological intervention with parent support.

A normal-phase isocratic chiral liquid chromatographic method has been developed and validated for atomoxetine hydrochloride. In addition to the S-enantiomer of atomoxetine, the conditions separate both para and meta positional isomers and the phenyl des-methyl analog. Method development strateg...

BackgroundDespite the recent progress of perinatal medicine, perinatal hypoxic-ischemic (HI) insult remains an important cause of brain injury in neonates, and is pathologically characterized by neuronal loss and the presence of microglia. Neurotransmitters, such as norepinephrine (NE) and gluta...