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Biomedical subjects

A Boucherle

Publications and source records attributed to A Boucherle.

At least 19 recordsLinked to original sources
PubMed1990

Drug-protein interactions. Comparative studies of levamisole and structural analogs or agents with immunomodulatory effect on the mechanism of protein aggregation.

Interactions of tetramisole, imidazo[2,1-b]thiazolic derived or immunomodulatory agents with human serum albumin (HSA) and immunoglobulins G and A has been investigated in vitro using polyacrylamide gel electrophoresis and immunoelectrophoresis. The results suggest that only the chemical structure type of tetramisole is able to induce a protein-protein interaction described as a mechanism of disulfide-sulfhydryl interchange reactions. The groups of atoms involved in the interaction are characterized.

Blood Proteins↗
PubMed1989

[Treatment of essential hypercholesterolemia by normolipidemic drugs in children].

The authors list the principal normolipidemic drugs. Only cholestyramine (Questran) and some fibrates (fenofibrate: Lipanthyl for instance) are registered for pediatrics. Cholestyramine acts by sequestering biliary acids, and thereby inhibiting intestinal cholesterol resorption. It is the primary drug used for children, when diet has been unable to restore normal cholesterol values.

Adolescent↗
PubMed1988

Drug-protein interactions. On the protein-protein interaction induced by levamisole in vitro. A mechanism hypothesis.

In the present communication, a model is reported in order to explain the aggregation of albumin induced by levamisole in vitro. The hypothesis suggests that the process of polymerization of albumins may include ligand-protein interaction as a biochemical catalysis, and covalent protein-protein interactions by a mechanism of disulfide-sulfhydryl interchange by intramolecular or intermolecular reactions.

Albumins↗
PubMed1988

Drug-protein interactions. A study of levamisole-serum albumin complex by 1H-NMR spectroscopy.

The chemical interaction of levamisole with human serum albumin (HSA) has been investigated using the technique of nuclear magnetic resonance spectroscopy. Binding to HSA occurs primarily with the imidazolidine and thiazolidine groups of levamisole as it has been demonstrated by selective changes in the relaxation times and the chemical shifts of the protons attached to the carbon atoms. The complex appears as the result of a weak linkage and may play a primordial role in the protein-protein interaction.

Humans↗
PubMed1986

[Contribution of stereochemistry to the study of the spatial organization of pharmacological receptors].

The important discovery by Pasteur of optical isomerism and the recent developments of stereochemistry showed that a complementarity exist between the geometry of molecules and their pharmacological receptors. The stereochemical bases and the principal configurational nomenclatures are briefly overviewed. The stereospecificity of the biological response and theories leading to an approach to stereochemical structures of main pharmacological receptors are developed. So, the biological activity of steroids is due to junctional modes of cycles and alpha or beta configurations of substituents. Acetylcholine has a skew conformation but it react by an anticlinal/anti-planar conformation with muscarinic receptor. To explain the difference in activity of adrenaline enantiomers, Easson and Stedman proposed a "three points" fixation to the adrenergic receptor. Dopaminergic receptor present a good degree of stereoselectivity: dopamine act by an anti-planar conformation in which the N-O distance is the same as in apomorphine (N-O10). The analgesic activity of morphinans is due to a cis junction of B and C cycles and to the stereoelectronic effect of the unshared lone pair on nitrogen. In the cyclamate sweeteners, some authors proposed for the sweet taste receptor a model with two points fixation (one acceptor and one donor) and two spatial barriers located at precise distances from this two sites. The stereoselectivity of molecules acting as substrates or inhibitors of enzymes is described. For example some oxazolidinone derivatives showed a selective inhibition toward monoamine oxidase A. Finally, the pharmacological activity falls often when molecules are administrated in racemic form. It seems that xenobiotics need to be dissymmetric for chiral recognition by biological systems.

Animals↗
PubMed1984

Toxicity and QSAR of chlorophenols on Lebistes reticulatus.

The 24-h toxicity of 20 substituted chlorophenols upon Lebistes reticulatus has been determined. The biological results have been tentatively connected with several of the following six parameters: logarithm of the octanol-water partition coefficient (log P); index of molecular connectivity (1 chi v); molecular refraction (RM); perimeter of the efficient section of the molecule (sigma D); constants of HAMMET (sigma); and melting point (F). A correlation is achieved using sigma D and sigma D2 with a correlation coefficient of 0.943.

Animals↗
PubMed1984

[N-aryl pyrrole derivatives with analgesic and anti-inflammatory activity 2. Pharmacologic modulation of the 1-arylpyrrole model].

In order to increase the pharmacological activities of the molecules described in the first part of the paper, an acetic or a 2-propionic group was introduced in to the fundamental structure, either on the aromatic ring, on the pyrrole nitrogen or on carbon 3 of the heterocycle. Moreover, a 4-chlorobenzoyl group was fixed on carbon 3 of the pyrrole via condensation of 4-chloroaniline with 4-chlorobenzoyl triketones. The structure of the adducts was demonstrated both by N.M.R. spectra and by using another unambiguous synthetic route. Finally, derivatives with the salicylic substructure on the nitrogen of the pyrrole are described. Their analgesic and anti-inflammatory properties are reported as well as some effects on the central nervous system.

Animals↗
PubMed1984

[N-aryl pyrrol derivatives with analgesic and anti-inflammatory activity. 1. 1-Arylpyrroles substituted at positions 4 and 5].

The derivatives in question are prepared by reaction of substituted anilines with 1,4-ketones in an acidic medium. The diketones are themselves obtained either using Friedel and Crafts reaction with levulinic acid chloride, or by Stetter's method reacting Mannich bases with aryl aldehydes in the presence of sodium cyanide. The results of test of acute toxicity and of analgesic and anti-inflammatory activity are reported.

Analgesics↗
PubMed1984

Drug-protein interactions. Inhibition of the action of levamisole on human serum albumin in vitro by DL-2-oxo-3-(2-mercaptoethyl)-5-phenyl-imidazolidine.

Comparative studies by polyacrylamide gel electrophoresis and immunoelectrophoresis showed that DL-2-oxo-3-(2-mercaptoethyl)-5-phenyl-imidazolidine (OMPI), a major metabolite of levamisole in vivo, exerted an inhibitory effect on the polymerization of albumin induced by levamisole action on human serum in vitro. Similar effects were obtained with sulfhydryl reagents. D-Penicillamine did not indicate such an action. The findings suggest that the SH groups of albumin may be involved in its interaction with levamisole.

Biopolymers↗
PubMed1983

[QSAR and aromatic series: proposals for steric parameters].

A steric parameter, sigma D (the perimeter of the efficacious section of a molecule in the same plane as the aromatic ring) is proposed. A comparison between sigma D, RM and 1Xv in six different series of aromatic molecules was made. In most cases the new parameter is preferable.

Animals↗
PubMed1982

Drug -- protein interactions in vitro. Effect of levamisole on human serum albumin.

The actions of (--)-2,3,5,6-tetrahydro-6-phenylimidazo[2,1-b]thiazole (levamisole) on human serum, human serum albumin (HSA) and bovin serum albumin (BSA) were studied. Analysis by polyacrylamide gel electrophoresis and immunodiffusion on gelose revealed the presence of aggregate forms of albumin in the human serum and a quantitative variation of polymeric forms with supplementary induced forms in case of HSA and BSA. The effect of other compounds with levamisole-like chemical groups including SH group or thiazolidine ring was investigated in similar conditions; aggregates were not observed. When the human serum was treated with these compounds, analysis by immunoelectrophoresis did not indicate a morphological change of lines of precipitate of immunoglobulins G and A previously described for levamisole action. The polymerization of albumin induced by the levamisole has been discussed. The whole of the data suggests that this drug may act in a specific way on the protein structure.

Animals↗
PubMed1981

Drug protein interactions.

Effects of two antirheumatic drugs, D-penicillamine and (-)-2,3,5,6-tetrahydro-6-phenylimidazo[2,1-b] thiazole (levamisole), on some human serum proteins with specific function are reported. Drug effects on the interaction corticosterone-corticosteroid binding globulin (CBG) in vitro were investigated especially by polyacrylamide gel electrophoresis. A quantitative modification of the % of corticosterone bound to CBG was noted. Drug effects on immunoglobulins involved in immune processes are described. Comparative studies by polyacrylamide gel electrophoresis and immunoelectrophoresis showed that addition of levamisole to the serum in vitro may give results different from those obtained when D-penicillamine was added. D-Penicillamine treatment was shown to induce principally a modification of Ig M, whereas levamisole caused a modification of Ig G and Ig A. On the other hand, "abnormal" fractions were noted by disc polyacrylamide gel electrophoresis when the serum was incubated with levamisole.

Anti-Inflammatory Agents↗