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Biomedical subjects

B Penicaut

Publications and source records attributed to B Penicaut.

7 recordsLinked to original sources
PubMed1997

Cholinesterase inhibition by derivatives of 2-amino-4,6-dimethylpyridine.

Derivatives of 2-amino-4,6-dimethylpyridine, aryl(alkyl)carboxamides, thiocarbamides and amidrazones, already known for their anti-inflammatory properties, were found to be moderately active inhibitors of acetyl and butyrylcholinesterase. Quantitative structure-activity relationships showed that the binding affinity was enhanced by the following structural modifications: (1) increase in molecular volume, (2) decrease in the energy of the lowest unoccupied molecular orbital, (3) insertion of a methylene group between the amide carbonyl and the aromatic ring, (4) replacement of the amide oxygen by sulfur. The affinity remained, however, weaker than that of the specific inhibitor 9-amino-1,2,3,4-tetrahydroacridine (tacrine). The association of anti-inflammatory and cholinesterase inhibiting activities within the same compound may prove useful for the treatment of Alzheimer's disease.

Acetylcholinesterase↗
PubMed1990

Acetylcholinesterase inhibition by two phosphoric 4-nitroanilides.

Two phosphoric 4-nitroanilides Z2P(O)NH-phi-NO2 (A, Z = Me; B, Z = NMe2) have been prepared and purified by chromatographic techniques. Their spectral data (uv, ir and 1H-nmr) have been determined, and compared with those of other similar compounds. Their ability to inhibit acetylcholinesterase has been measured by a modification of Ellman's method. The data, as computed according to the Michaelis scheme, indicate that A is not an inhibitor, whereas B is a reversible mixed one. These differences are discussed in terms of hydrophobic interactions.

Acetylcholinesterase↗
PubMed1990

[Plasma kinetics of a spiroarsorane trypanocidal agent in sheep trypanosomiasis].

In a previous study, spiroarsoranes were very effective against both the two pathogenic phases of the experimental sheep trypanosomiasis. In this paper, the authors had studied the plasmatic pharmacokinetics of these compounds. Data had shown one peak 10 min after injection of a 3 months inoculated sheep, and 90 min for the control sheep. Spiroarsorane had a good diffusion into the central nervous system, but the trypanocidal activity, during the second phase of the disease, was effective only after repeated treatment. The spiroarsorane low toxicity could allow its direction against nervous trypanosomiasis.

Animals↗
PubMed1990

[Trypanocidal activity and plasma kinetics of cis-Pt(II) pentamidine in the parasitized sheep].

The trypanocidal activity of cis-Pt(II) pentamidine had been demonstrated during the first phase of Trypanosoma brucei brucei sheep experimental trypanosomiasis. But a subcutaneous treatment with 5 mg.kg-1 (+2 x 12 mg.kg-1) was not effective during the brain phase of trypanosomiasis. The blood pharmacokinetics of this compound had a plasmatic peak between 45 and 60 min, followed by a low decreasing phase along several days. The curve shape allowed an important interval before the following injection, and showed a compound storage in internal organs and extravascular sites. A model of cis-Pt(II) pentamidine metabolism had been studied: this product could be used as a chemoprophylactic medicine against African trypanosomiasis and American leishmaniasis.

Animals↗
PubMed1986

[Comparative study of the toxicity of metal chlorides and a synthetic organic molluscacide, N-tritylmorpholine, in 2 fresh-water amphipods, Gammarus pulex and Echinogammarus berilloni].

The effects of three metal salts (BaCl2, CuCl2, ZnCl2) and of N-trityl-morpholine (Triphenmorph) were studied on two aquatic amphipod species, Gammarus pulex and Echinogammarus berilloni. Experiments were made up in eucalcic and oligocalcic waters for determining the LC50 at different exposure times. The order of toxicity was the same in eucalcic water with the two species: Triphenmorph greater than Cu2+ greater than Zn2+ greater than Ba2+. This order was the same in oligocalcic water with Echinogammarus berilloni; with Gammarus pulex, CuCl2 was more toxic than Triphenmorph.

Animals↗
PubMed1983

[Pharmacokinetics and urinary metabolism of albendazole in man].

Albendazole, a new broad spectrum benzimidazole anthelmintic, has been administered in 10 male volunteers. Administration was randomized using 100 mg tablets, 200 mg tablets and a 2% suspension. Blood samples were obtained 0.5; 1; 1.5; 2; 2.5; 3; 3.5; 4; 5; 6; 8; 12; 24; 72 h after treatment. Albendazole sulfoxide, one of the mains albendazole blood metabolites, was assayed by HPLC and the blood half life was calculated as 8 1/2 h. The three different pharmaceutical formulations were considered bioequivalent. Urines were collected, and using T. L. C. Technics, main metabolites were identified and characterized. Hydrolysis of the carbamate function and oxidation of the sulfur atom, the alkyle chain and the aromatic ring were the main biotransformations observed.

Adult↗