A series of terminal nonyl chain and nucleobase modified analogues of (+)-EHNA (III) were synthesized and evaluated for their ability to inhibit adenosine deaminase (ADA). The constrained carbon analogues of (+)-EHNA, 7a-7h, 10a-c, 12, 13, 14 and 17a-c appeared very potent with Ki values in the ...

Analogues of 3,4-dimethyl-4-(3-hydroxyphenyl)piperidines are high affinity inverse agonists for μ-, δ- and κ-opioid receptors. To characterize inverse agonist binding, we synthesized a high specific activity radioligand from this series, [3H]LY515300 (3-[1-((3-cyclohexyl-[3,4-3H2])-3(R,S)-hyd...

(R)-3,5-Bistrifluoromethylphenyl ethanol 2, a key building block in the synthesis of aprepitant, has been synthesized from ketone 5 via catalytic asymmetric transfer hydrogenation using a simplified catalyst generation procedure. The process uses (1S,2R)-cis-1-aminoindan-2-ol 10 and dichloro(p-c...

(S)-3,5-bistrifluoromethylphenyl ethanol is a key chiral intermediate for the synthesis of NK-1 receptor antagonists. Enantioselective synthesis of (S)-3,5-bistrifluoromethylphenyl ethanol was successfully performed in high enantiomeric excess (e.e.) through asymmetric reduction of 3,5-bis(trifl...

The synthesis of (S)-3,5-bistrifluoromethylphenyl ethanol, a pharmaceutically important alcohol intermediate for the synthesis of NK-1 receptor antagonists, was demonstrated from a ketone via asymmetric enzymatic reduction. The isolated enzyme alcohol dehydrogenase from Rhodococcus erythropolis ...

A total of 82 fungal isolates were screened for their ability to reduce 3,5-bis(trifluoromethyl)-acetophenone 1. Penicillium expansum was found to successfully reduce ketone 1 in the submerged culture. A second screening was performed on the active P. expansum strains identified by the first scr...

Two methods for automated analysis of extracts from edible muscle tissue of Atlantic salmon are described. Oxolinic acid and flumequine are extracted with phosphate buffer pH 9, and the extracts are analysed by high-performance liquid chromatography using a column-switching system. One method ap...

A simple high-performance liquid chromatographic method for assaying oxolinic acid, a chemotherapeutic agent, in fish tissues has been developed. Nalidixic acid is used as an internal standard. The drugs are separated on an internal surface reversed-phase column. The sample clean-up is minimized...

SummaryThe place occupied by fluoroquinolones is very important clinically. Ciprofloxacin has been the most widely prescribed one which exhibits good activity against Pseudomonas aeruginosa and Acinetobacter. D-glucose is frequently used as an excipient in most formulations for perfusion solutio...

A simple procedure for the determination of oxolinic acid (OA) and oxytetracycline (OTC), two antibacterial agents, in the shell of the blue mussel (Mytilus edulis), using reversed-phase high-performance liquid chromatography is described. Liquid chromatography was performed on a 5-μm LiChroSph...

The neutral mononuclear copper complexes with the quinolone antibacterial drug oxolinic acid in the presence or not of a nitrogen donor heterocyclic ligand 1,10-phenanthroline, 2,2′-bipyridine or 2,2′-dipyridylamine have been synthesized and characterized with infrared, UV-visible and electron...

The present study demonstrates photoinduced generation of superoxide radical anion and singlet oxygen upon UVA irradiation of ethyl 1,4-dihydro-8-nitro-4-oxoquinoline-3-carboxylate (DNQC), and its cytotoxic/phototoxic effects on murine leukemia L1210 cells. The formation of reactive oxygen speci...

Ethyl 2-ethenyl-6,7-methylenedioxy-1,2,3,4,-tetrahydro-1-(3′,4′,5′-trimethoxyphenyl)-4-oxoquinoline-3-carboxylate 1 was prepared by the reaction of vinylcuprate on ethyl 1,4-dihydro-6,7-methylenedioxy-1-(3′,4′,5′-trimethoxyphenyl)-4-oxoquinoline-3-carboxylate 9. Different quinolones and a ...

Characteristics of 3′-monoiodothyronine (3′-T1) degradation were examined in vitro in rat tissue homogenates. In rat liver homogenates, 3′-T1 degradation was optimal at pH 7.4, and was dependent upon time, temperature, and tissue concentration. The Michaeli's constant (Km) = 0.84 μmol/L...

A new route for the preparation of radioactively labelled α-methyl l-tyrosine is described. The labelling at the α position has been successfully achieved with 14C-, 11C- (very preliminary, unpublished), and 3H-labelled methyl iodide. A detailed report on 14C-labelling at the α position and t...

Characteristics of the irreversible binding of cytembena (CYT) to rat liver microsomal proteins have been investigated in vitro. Binding of [14C]CYT to rat liver microsomal proteins remained unchanged in the presence of SKF-525A or after heat denaturation and was not dependent upon the presence ...

Cytogenetic analysis and the micronucleus test of bone-marrow cells was used to study the possible extrapolation of results from experimental animals to man.Cytembena was given i.p. in doses of 5, 10, 20, 40 and 80 mg/kg body wt. to Wistar rats in doses of 20, 40 and 80 mg/kg body wt. to ICR mic...

Cytembena (cis-β-4-methoxybenzoyl-β-bromoacrylic acid, NSC-104, 801) has been tested for its anticancer activity. One complication to its use is the possibility of drug-induced nephrotoxicity. The present study was designed to characterize further the nature of the renal damage. Rats injected ...

Cyclic voltammetry and controlled potential electrolysis were used to show that radical anions of 2- and 4-nitrophenylhydroxylamines electrochemically generated in a 0.1 M Bu4NClO4 solution in DMF undergo protonation with the starting compounds (self-protonation) followed by the formation of the...

Based on controlled potential electrolysis and cyclic voltammetry, the chain reaction of 4,4′-dinitroazobenzene formation was shown to be initiated during the electrochemical reduction of 4-nitrophenylhydroxylamine in DMF.