Background. – Actomyosin ATPase is one of the major ATP consuming enzymes in the myocardium. We tested whether 2,3-butanedione monoxime (BDM), a reversible inhibitor of actomyosin ATPase, given before coronary occlusion, limits infarct size in anesthetized open-chest dogs.Methods and results. –...
Simple and selective single-step synthesis of 5-ethyl-2-methylpyridine (EMP) under high pressure (autogeneous pressure) conditions is achieved with high conversion and high selectivity over zeolites. The catalyst can be reused many times without significant loss of activity.
4,5-Dimthexycanthin-6-one and 5-hydroxy-4-methoxycanthin-6-one are the main active ingredients of Picrasma quassioides, which is a widely used herbal medicine for the treatment of gastroenteritis, snakebite, infection and hypertension in China. In the present study, the in vitro metabolites of 4...
4,5-Dimethoxycanthin-6-one and 5-hydroxy-4-methoxycanthin-6-one are the active ingredients of P. quassiodes. In the present work, a LC–MS/MS method was developed for the determination of 4,5-dimethoxycanthin-6-one and its major metabolites 5-hydroxy-4-methoxycanthin-6-one (M1) and 4-hydroxy-5-m...
Intermolecular hydroarylation of propynoic acid and its esters with indoles proceeded efficiently in acetic acid under a catalytic system of FeCl3/3AgOTf and afforded the corresponding 3,3-bis(indol-3yl)propanoic acids and their esters in high yields. In the case of 2-methylindole, 3-indolylacry...
A direct and selective method for the α,β-dehydrogenation of esters using palladium catalysis in the presence of free OH and NH functionalities is reported herein. Allyl-palladium catalysis allows for preservation of readily oxidizable functionalities such as amines and alcohols. Furthermore, ...
In the present study we have performed comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) on structurally diverse ligands of Ah (dioxin) receptor to explore the physico-chemical requirements for binding. All CoMFA and CoMSIA models have gi...
2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD) is a potent inducer of hepatic microsomal enzymes. The influence of an inducing dose of TCDD on tissue distribution and other pharmacokinetic behavior of a TCDD analog in the mice was examined by employing a high specific activity radioligand, [125I]-2-...
Two optimized pranoprofen-loaded poly-l-lactic-co glycolic acid (PLGA) nanoparticles (PF-F1NPs; PF-F2NPs) have been developed and further dispersed into hydrogels for the production of semi-solid formulations intended for ocular administration. The optimized PF-NP suspensions were dispersed in f...
One new metal coordination polymer constructed from Pranoprofen drug ligand, namely, [Co(L)2]n (or 1) (HL = 2-(5H-chromeno[2,3-b]pyridin-7-yl) propanoic acid), has been obtained by the solvothermal reaction, which was characterized by element analyses, FT-IR, X-ray single-crystal diffraction, po...
A comparative degradation of sodium dodecyl sulfate (SDS) by photoelectrochemical (PEC) and electrochemical in dark (EC – dark) processes was investigated. The completed degradation of SDS molecules after the first hour was observed via UV–Vis spectrum and Fourier transform infrared spectrosco...
Different Tetraalkylammonium (TAA+) counterions including tetramethylammonium (TMA+), tetraethylammonium (TEA+), tetrapropylammonium (TPA+) and tetrabutylammonium (TBA+) with dodecyl sulfate (DS−) at the air/water interface were studied with atom molecular dynamics (MD) simulations. Structural p...
A series of double selenates, as (CH3)4NLn(SeO4)24H2O (Ln = Rare earth ion like La, Pr, Nd, Sm, Gd, Tb, Dy) was crystallized from mixed solution and characterized in detail for their structure, vibrational and optical properties as well as thermal stabilities. The crystal structure of the praseo...
Cobalt electrodeposition was carried out in Watts type bath to investigate the effects of sodium saccharin and tetramethylammonium bromide on the crystal structure, morphology, surface roughness and microhardness of thick cobalt deposits. The addition of sodium saccharin changed the crystal orie...
The deoxyuridine suppression test was performed on isolated rat bone marrow cells in order to study the effect of bidisomide, a new Class I antiarrhythmic agent, on folate-dependent DNA synthesis. Methotrexate and 5-fluorouracil, two known inhibitors of DNA synthesis, were included in the study ...
The structural investigations of the molecular complex of 2-methyl-4-nitroaniline with trichloroacetic acid, namely 2-methyl-4-nitroanilinium trichloroacetate trichloroacetic acid (C11H10Cl6N2O6) have been performed by means of single crystal and powder X-ray diffraction method. The complex was ...
Factor Xa is a serine protease representing a crucial element in the coagulation process and an attractive target for anticoagulant therapy. At the present time there are several chemical classes of factor Xa inhibitors with proven activity. Furthermore, three factor Xa inhibitors have been appr...
Novel conjugates of purine and 2-aminopurine linked with heterocyclic amines, including chiral derivatives of 3,4-dihydro-2H-[1,4]benzoxazine, 3,4-dihydro-2H-[1,4]benzothiazine and 1,2,3,4-tetrahydroquinoline, by 6-aminohexanoyl fragment at the 6-position of purine moiety were obtained. For this...
The acylative kinetic resolution of racemic 6-fluoro-2-methyl-1,2,3,4-tetrahydroquinoline, 7,8-difluoro-3,4-dihydro-3-methyl-2H-[1,4]benzoxazine, and their non-fluorinated analogues with (S)-naproxen and N-phthaloyl-(S)-amino acyl chlorides has been carried out. It has been shown that the presen...
Reversed-phase high performance liquid chromatographic methods for the analysis of ointments containing hydrocortisone and clioquinol have been investigated. A successful method using a C18 column and methanol-0.05 M phosphoric acid (80:20) as eluting solvent has been developed which allows both...
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