8-Chloro-6-(3-dimethylaminopropylamino)-11H-pyrido[2,3-b][1,4]benzodiazepine

in Acta Crystallographica Section E-Structure Reports Online (2002), 58(Part 1), 69-71

The crystal structure determination of the title compound, C17H20ClN5, has been undertaken as part of studies on antipsychotic drugs. Its structure is compared with that of clozapine (C18H19ClN4), a well ... [more ▼]

The crystal structure determination of the title compound, C17H20ClN5, has been undertaken as part of studies on antipsychotic drugs. Its structure is compared with that of clozapine (C18H19ClN4), a well known atypical antipsychotic drug. The side chain is more flexible than in the N-methylpiperazine analogues, but its folding is influenced by an intramolecular N-H . . .N hydrogen bond. The distances between the N-distal atom, a possible pharmacophore, and the centres of the two aromatic rings are significantly shorter than in clozapine. The crystal packing involves one N-H . . .N intermolecular hydrogen bond. The title compound showed no affinity for the receptors tested. [less ▲]

Inhibition by JL3 of some effects of histamine and of the anaphylactoid reactions induced by dextran in rats.

Poster (2001)

Anti-inflammatory and chondroprotective activity of prodelphinidins isolated from Ribes nigrum leaves.

Poster (2000)

Study of the Influence of Both Cyclodextrins and L-Lysine on the Aqueous Solubility of Nimesulide; Isolation and Characterization of Nimesulide-L-Lysine-Cyclodextrin Complexes

in Journal of Pharmaceutical Sciences (1997), 86(4), 475-80

Nimesulide is a nonsteroidal antiinflammatory drug that exhibits a very poor water solubility (0.01 mg.mL-1). A nimesulide-beta-cyclodextrin complex prepared according to patent application WO 94/ 02177 ... [more ▼]

Nimesulide is a nonsteroidal antiinflammatory drug that exhibits a very poor water solubility (0.01 mg.mL-1). A nimesulide-beta-cyclodextrin complex prepared according to patent application WO 94/ 02177 has an aqueous solubility of approximately 16 mg.mL-1 of nimesulide. A nimesulide-L-lysine salt has also been prepared and increases the aqueous solubility of nimesulide to approximately 5.0-7.5 mg.mL-1. The purpose of the present study was to investigate the interaction of both cyclodextrins and L-lysine on the aqueous solubility of nimesulide. Nimesulide-L-lysine-beta- or gamma-cyclodextrin complexes were prepared by spray-drying. The inclusion of the nimesulide-L-lysine salt into the cyclodextrin cavity was confirmed by differential scanning calorimetry and proton nuclear magnetic resonance spectroscopy. These complexes offered remarkable aqueous solubility. The incorporation of nimesulide in a nimesulide-L-lysine-beta-cyclodextrin complex increased its water solubility by a factor of 10 at pH 1.5 (0.050 mg.mL-1 for the complex versus 0.005 mg.mL-1 for nimesulide), 160 at pH 6.8 (2.373 mg.mL-1 for the complex versus 0.015 mg.mL-1 for nimesulide), and 3600 in purified water (36.400 mg.mL-1 for the complex versus 0.01 mg.mL-1 for nimesulide). [less ▲]

Study of the influence of g-cyclodextrin on the molsidomine photostability

Poster (1996, April)

Dibenzoazepine analogues : the electrophysiological properties of JL3, a potential atypical antidepressant

in European Journal of Pharmacology (1996), 310

Les activateurs de canaux potassiques: étude structurale comparative du pinacidil, du diazoxide et du cromakalim

in Annales Pharmaceutiques Françaises (1995), 53(5), 201-8

A conformational analysis has been performed with SYBYL starting from the energy optimized (Tripos force field) X-ray conformation of (R,S)-pinacidil. The geometry of four selected low energy conformers ... [more ▼]

A conformational analysis has been performed with SYBYL starting from the energy optimized (Tripos force field) X-ray conformation of (R,S)-pinacidil. The geometry of four selected low energy conformers has been reoptimized using the AM1 semiempirical Molecular Orbital method (MOPAC 5.0), and the total energy of the optimized conformers has been compared. In spite of an apparent structural dissimilarity, a good analogy has been found between the calculated isopotential map of diazoxide and that of at least one selected low energy conformer of pinacidil. It has been suggested that, unlike cromakalim, the low but observable activity of pinacidil on pancreatic B-cells could be explained by adoption for this compound of a conformation having a diazoxide-like stereoelectronical imprint which could assume a similar interaction on the same biological receptor. [less ▲]

Synthèse de dérivés 3-aminoaralkyl-2-aryl-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxydes et leur évaluation en tant qu'antagonistes de la cholécystokinine

in Journal de Pharmacie de Belgique (1995), 50

Synthèse, étude théorique et évaluation biologique de dérivés du 4-amino-4H-1,2,4-triazole analogues des antibiotiques b-lactamiques

in European Journal of Medicinal Chemistry (1992), 27(3), 193-205

New alkoxypyridine Sulfonamides: Synthesis, Biological Evaluation and Physicochemical Properties

in Helvetica Chimica Acta (1991), 74