Study ObjectiveTo evaluate whether ramosetron increases the corrected QT (QTc) interval.

BackgroundSpinal anesthesia with intrathecal morphine is a reliable, easy to apply, and cost effective method for controlling pain after total knee arthroplasty (TKA). However, postoperative nausea and vomiting (PONV) is a major concern. 5-Hydroxytryptamine receptor 3 (5-HT3) antagonists like on...

4-Lithio and 4,6-dilithiodibenzothiophenes were efficiently obtained by lithiation of dibenzothiophene with BuLi and BuLi-TMEDA, respectively. Very pure 4-methyl- and 4,6-dimethyldibenzothiophenes, substrates of great request in hydrosulfurization studies were easily prepared, on large scale and...

Efficient kinetic resolution of racemic 2-aryl-3-nitro-2H-chromenes (1a–l) has been explored with the pyrrolidinyl-camphor derivative 2b as a bifunctional organocatalyst under neat conditions in the presence of AcOH at 0 °C. In general, the organocatalytic asymmetric Michael addition of ketone...

A series of bufalin 3-nitrogen-containing-ester derivatives (2–6) were designed, synthesized, and evaluated for their proliferation inhibition activities against human cervical epithelial adenocarcinoma (HeLa) and non-small-cell lung cancer (A549) cell lines. The structure–activity relationshi...

First ever synthesis of functionalized 5,7-dihydro-6H-dibenzo[d,f][1,3]diazepin-6-ones (6, 9) has been developed through base induced ring transformation of 2H-pyran-2-one-3-carbonitriles with indolin-2-ones. A protocol for alkenylating indolin-2-ones by 2H-pyran-2-one-3-carbonitriles has also b...

Novel derivatives of 6-fluoro-4-piperidinyl-1,2-benzisoxazole amides 4(I–VI) were obtained by the condensation of different acid chlorides with 6-fluoro-3-piperidin-4yl-benzo[d]isoxazole. Also, 6-fluoro-chroman-2-carboxamides 6(I–III) were synthesized by using nebulic acid chloride with differ...

A series of novel s-triazine analogs were synthesized and characterized by IR, 1H NMR, 13C NMR, 19F NMR spectroscopy and elemental analysis. Preliminary screening of target compounds against eight bacteria (Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Klebsie...

The worldwide prevalence of NDM-1-producing bacteria has drastically undermined the clinical efficacy of the last line antibiotic of carbapenems, prompting a need to devise effective strategy to preserve their clinical value. Our previous studies have shown that ebselen can restore the efficacy ...

s-Triazine is considered a privileged structure, as it is found in several FDA-approved drugs. In the framework of our ongoing medicinal chemistry project based on the use of s-triazine as a scaffold, we synthesized a series of mono- and di-pyrazolyl-s-triazine derivatives and tested them agains...

Piperidinyl-3-phosphinic acid 2, piperidinyl-3-methylphosphinic acid 3 and N-(4,4-diphenyl-3-butenyl)-piperidinyl-3-phosphinic acid 4 have been synthesized as bioisosteres of the corresponding amino carboxylic acids, which are potent and specific GABA-uptake inhibitors. The novel amino phosphini...

Here in, we report the preparation and evaluation of four 3-hydroxy-piperidine-N-benzyl-aryl-acylhydrazone derivatives (6a–d) for their potential antinociceptive activity. In the tail flick test, compounds 6a and 6d exhibited a significant increase in the latency time of the animals, in compari...

One of the experimental programs that will be carried out at the Extreme Light Infrastructure – Nuclear Physics (ELI-NP) facility is the production of exotic neutron-rich ion beams in an IGISOL facility via photofission in a stack of actinide targets placed at the center of a cell filled with H...

NP-252, a new dihydropyridine derivative, and nifedipine non-competitively inhibited contractile responses to KCl and responses to Ca2+ in Ca2+-free medium containing KCl in rabbit aorta and renal, mesenteric, coronary and basilar arteries, mesenteric veins and vena cava. The effects of NP-252 i...

A facile and economical hydrothermal approach is reported for preparing fluorescent nitrogen-doped carbon dots (N-CDs) via using o-phenylenediamine and dicyandiamine. Herein, the bright-yellow-emissive N-CDs are uniformly dispersed spherical nanoparticles with favorable solubility, superior phot...

The vasoinhibitory effect of NP-252, a 1,4-dihydropyridine derivative Ca++ antagonist, was examined in canine cerebral artery, and this effect was compared with that of nifedipine. NP-252 (10−7 M) and nifedipine (10−6 M) nearly abolished the contraction induced by addition of Ca++ to Ca++-free m...

Sphingosine has been shown to be a potent and specific inhibitor of protein kinase C in vitro and in cell systems including human platelets. Questions have been raised as to the validity of commercial sphingosine as a protein kinase C inhibitor and whether sphingosine or N,N-dimethylsphingosine ...

A ruthenium complex [RuL1Cl2(PPh3)]Cl (L1 = (E)-2-((pyridine-2-yl)methyleneamino)benzoic(E) acid) was synthesized, characterized by analytical techniques, and then it has been employed as chemo-sensor for the recognition of acetate in H2O:CH3CN (80:20) medium. With fluorescence study, it has bee...

We have previously demonstrated that monatepil maleate, AJ-2615, a new calcium antagonist endowed with α1-adrenoceptor blocking property, has antiatherosclerotic and plasma lipid-lowering effects in Japanese monkeys fed on a cholesterol-rich diet. To clarify the mechanisms on plasma lipid-lower...

IntroductionIncreased ocular hypertension is one of the main characteristics of glaucoma. Monatepil belongs to a class of calcium channel blockers with special characteristic of α1-adrenergic receptor blocking effect. Calcium channel blockers and α1-adrenergic receptor blocker act as antihyper...