Thiol-thione tautomerism of 1,2,4-triazole derivative with Schiff base was investigated by spectroscopic methods and quantum mechanical calculations. Theoretical study of thiol-thione tautomeric forms of 1,2,4-triazole derivative with Schiff base; 1,2,4-triazole-thiol form, 1-((5-mercapto-4-(thi...

The synthesis, spectroscopic characterization, reactivity study and evaluation of antioxidant and α-glucosidase inhibitory activities of two Schiff bases containing 1,2,4-triazole and pyrazole rings namely: 4-((4-methoxybenzylidene)amino)-5-(5-methyl-1H-pyrazol-3-yl)-4H-1,2,4-triazole-3-thiol 3...

4-amino-1,2,4-triazole derivatives; 4-amino-1-((5-mercapto-1,3,4-oxadiazole-2-yl)methyl)-3-(thiophene-2-ylmethyl)-1H-1,2,4-triazole-5(4H)-one (1) and 4-amino-1-((4-amino-5 mercapto-4H-1,2,4-triazole-3-yl)methyl)-3-(thiophene-2-ylmethyl)-1H-1,2,4-triazole-5(4H)-one (2) were studied theoretically ...

Sorcin (soluble resistance-related calcium-binding protein), an acidic (pI = 5.7) protein (Mr ∼ 20 kDa) previously designated V19, was originally identified in cells selected for high levels of resistance to vincristine. Two-dimensional gel electrophoresis and/or Western blot techniques now sho...

SUMMARYPapaveretum-hyoscine is a popular premedication for children but there is no agreement as to dosage. Four dosage schemes were compared in a double blind trial on children undergoing adenotonsillectomy in an attempt to determine the optimum method of using the drug mixture. No real differe...

Buprenorphine 0.3 mg and papaveretum 20 mg, both combined with hyoscine 0.4 mg, were used is premedicants in female patients undergoing laparoscopy or abdominal hysterectomy. The effects were compared. It was found that the increase in drowsiness and tranquillity was greater following buprenorph...

In this study, [125I] CGP 42112, a ligand of high affinity and selectivity for the angiotensin II AT2 receptor, was used to detect and quantify a non-angiotensin II binding site in the balloon-injured carotid artery of the rat. The amount of [125I] CGP 42112 binding was significantly enhanced in...

Most radiolabeled ligands for angiotensin II (Ang II) receptors do not discriminate between the AT1 and AT2 receptor subtypes, which must be distinguished by displacement with selective AT1 or AT2 ligands. We compared [125I]CGP 42112 with the non-selective agonist [125I]Sar1Angiotensin II. We st...

The synthesis of several cyclic amino acids that have all the necessary structural features to make them ideal scaffolds for use in medicinal chemistry is described. A key step in each synthesis is the use of hydrolase enzymes to define a chiral centre. In order to elaborate these building block...

The disposition of the non-steroidal anti-inflammatory drug (NSAID) nabumetone after a single oral dose administration of nabumetone tablets to humans and minipigs was investigated. Nabumetone is a prodrug, which is metabolized in the organism to the principal pharmacodynamically active metaboli...

Rhodium nanoparticles, derived from mesitylene-solvated rhodium atoms, deposited on γ-Al2O3, are excellent catalysts for the selective hydrogenation of the double bond in α,β-unsaturated carbonyl compounds. The low metal loading Rh on γ-Al2O3 catalyst, containing trioctylamine, TOA, as stabi...

A novel, rapid, simple and green vortex-assisted surfactant-enhanced emulsification microextraction method based on solidification of floating organic drop was developed for simultaneous separation/preconcentration and determination of ultra trace amounts of naproxen and nabumetone with high per...

A highly selective and sensitive colorimetric sensor for the determination of nabumetone (NAB) based on the aggregation of the thiolated β-cyclodextrin (Tβ-CD) functionalized gold nanoparticles (Au-NPs) with NAB in the presence of polyvinylpyrrolidone (PVP) was developed. Thiolated β-cyclodex...

Two efficient, simple, cheap, and environmentally benign preparations of cyclopropanes were achieved. One is the formation via 3-exo-trig manner from various electron-deficient 2-iodoethyl-substituted olefins with zinc powder in a mixture of t-butyl alcohol and water, and the other is the format...

O-carboxymethylchitosan (OCMC) microspheres containing an antibiotic drug pazufloxacin mesilate (PM) have been successfully prepared by emulsion cross-linking using glutaraldehyde (GA). Various manufacturing parameters, including amount of cross-linking agent and OCMC:PM ratios were altered to o...

AimThe present work aim to develop a simple, accurate and sensitive RP-HPLC method and validated for the estimation of pazufloxacin in pure drug and it's injectable dosage.

The present study examined the clinical pharmacokinetics of pazufloxacin in prostate tissue and estimated the probability of target attainment for tissue-specific pharmacodynamic goals related to treating prostatitis using various intravenous dosing regimens. Patients with prostatic hypertrophy ...

A novel colorimetric nanomaterial-assisted optical sensor for pazufloxacin mesilate was proposed for the first time. Pazufloxacin mesilate could induce the aggregation of glucose-reduced gold nanoparticles (AuNPs) through hydrogen-bonding interaction and electrostatic attraction, leading to the ...

Culicinin D is a 10 amino acid peptaibol containing a rare and synthetically challenging (2S,4S,6R)-AHMOD residue, that exhibits potent antiproliferative activity against MDA-MB-468 cells. An SAR study focusing on replacement of the AHMOD residue was undertaken, culminating in the revelation tha...

To understand the biological function of taurine, a study of taurine kinetics in the cat was undertaken. This paper describes a method developed for the accurate determination of 15N-taurine enrichment in cat urine by gas chromatography—mass spectrometry. 15N-Taurine was given to six animals as...