The synthesis of benzothiazolium salt, N-(carboxyethyl)-2-methylbenzothiazolium bromide has been carried out by condensation of 2-methylbenzothiazole and 3-bromopropionic acid in solvent free conditions. The desired compound was obtained in excellent yield and its structural characterization was...

PurposeThe objective of this study was to evaluate the efficacy and safety of the lercanidipine/valsartan combination compared with lercanidipine monotherapy in patients with hypertension.

Lercanidipine (LERCA) is a third generation antihypertensive drug belonging to the 1,4-dihydropyridine’s family, which has been reported to induce photoallergic and/or phototoxic effects in patients with long term treatment. The electronic nature of substituents on the 4-aryl moiety bonded to t...

Oxidative stress, inflammation and apoptotic neuronal cell death are cardinal mechanisms involved in the cascade of acute ischemic stroke. Lercanidipine apart from calcium channel blocking activity possesses anti-oxidant, anti-inflammatory and anti-apoptotic properties. In the present study, we ...

The objective of this study was to develop lercanidipine–hydroxypropylmethyl cellulose (HPMC) nanoparticles with high oral bioavailability. The lercanidipine–HPMC nanoparticles with/without surfactants were manufactured using a supercritical antisolvent (SAS) process. Gelucire 44/14, poloxamer...

A series of pyrrolo[2,3-b]pyridine derivatives bearing the 1,8-naphthyridin-2-one moiety were synthesized, and evaluated for their antiproliferative activity against four cancer cell lines (HT-29, A549, H460, and U87MG) and six tyrosine kinases (c-Met, Flt-3, PDGFR-β, VEGFR-2, EGFR, and c-Kit) ...

A series of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing the 1,8-naphthyridin-2-one moiety were designed, synthesized and evaluated for their biological activities. The target compounds exhibited moderate to high antiproliferative activity against three cancer cell lines (A549, HepG2...

The apical sodium--dependent bile acid transporter (ASBT) is the main transporter to promote re-absorption of bile acids from the intestinal tract into the enterohepatic circulation. Inhibition of ASBT could increase the excretion of bile acids, thus increasing bile acid synthesis and consequent...

A series of 1-[4-(substituted phenyl)-2-(substituted phenyl azomethyl)-benzo[b]-[1,4]diazepin-1-yl]-2-substituted phenylaminoethanones (1–17) was synthesized and evaluated in vitro for its antimicrobial and anticancer activities. Results of antimicrobial screening indicated that 1-[4-[4-Chloro-...

An effective, asymmetric total synthesis of the antibiotic (+)-sorangicin A (1) has been achieved. Central to this venture was the development of first- and second-generation syntheses of the signature dioxabicyclo[3.2.1]octane core, the first featuring chemo- and stereoselective epoxide ring op...

In this paper, we disclose the synthesis of the dioxabicyclo[3.2.1]octane subunit of the potent antibiotic sorangicin A. The synthesis was achieved in a convergent manner in 8 steps. Regio- and stereoselective intermolecular epoxide opening, ring-closing metathesis and iodo-etherification are ke...

Synthesis of [18F]4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide ([18F]celecoxib), a selective COX-2 inhibitor, is achieved via a bromide to [18F]F− exchange reaction. Synthesis of the precursor for radiolabeling was achieved from 4′-methylacetophenone in four step...

The crystal structures of C23H20N2O3 (I) and C22H18N2O2 (II) have been determined by single-crystal X-ray diffraction. These two compounds crystallise in the monoclinic space groups, P21c and C2c. The structures have been determined by direct methods and refined to R, 0.041 (I) and 0.070 (II). T...

Mitochondria is a main organelle for conducting aerobic respiration in the process of metabolism. Deoxyribonucleic acid (DNA) plays central roles in the genetic encoding, regulation and expression in the living normal and cancer cells. However, imaging of mitochondria and DNA in biological syste...

In this study, effects of manganese and magnesium content on the electrochemical properties of Al-Zn-ln sacrificial anode were studied in 0.5 mol/L NaCI solution (pH=5). The aluminum base alloy with different amounts of Mn and Mg were melted at 750°C, then casted at molds at 25°C. Corrosion ex...

Coordination compounds of titanium (IV) and zirconium (IV) with tetra-aryl-1,3-dioxolan-4,5-dimethanol (1,2) derivatives were synthesized and characterized by NMR- and IR-spectroscopy and X-ray crystallography. It was demonstrated that titanium dichloride complexes (5–6, 9–12) when treated wit...

To understand the effect of precipitation pH and coexisting Mg2 + on phosphate adsorption onto zirconium oxide (ZrO2), ZrO2 particles precipitated at pH 5.3, 7.1 and 10.5, i.e., ZrO2(5.3), ZrO2(7.1) and ZrO2(10.5), respectively were prepared and characterized, then their adsorption performance a...

In the present work, hydroxyapatite (HAP)-based plasma electrolytic oxide (PEO) coatings were produced on zirconium at different current densities in a solution containing calcium acetate and β-calcium glycerophosphate by a single step. The phase structure, surface morphology, functional groups...

Zirconium phosphate (ZrP) and its organic derivative, zirconium phosphonate, increasingly attract research interest due to their outstanding physical and chemical properties, both in their amorphous and in their crystalline phases. These include an extremely high ion-exchange capability, high as...

Anodic dissolution behavior of zirconium in Bun4NBr-contaning isopropanol solution was investigated using cyclic voltammetry, linear sweep voltammetry and chronoamperometry, complemented with a scanning electron microscope (SEM). The voltammograms did not exhibit active dissolution until the bre...