Evaluation de la sélectivité COX-1 vs COX-2 de drogues à potentialités anti-inflammatoires

Poster (1999, May)

Derivatives of 2,5- and 3,5-disubstituted anilines, their preparation and use

Patent (1999)

The effect of hydroxypropyl-b-cyclodextrins on the pharamacokinetics of albendazole in sheep

in Proceedings of 26th International Symposium on Controlled Release of Bioactive Materials (1999)

Pharmacological evaluation of 3-alkylsulfanyl-4H-1,2,4-benzothiadiazine 1,1-dioxides structurally related to the KATP channel opener diazoxide

in Fundamental & Clinical Pharmacology (1999), 13

Effective resolution of racemic pirlindole at the preparative scale

in Chirality (1999), 11

Synthesis and structural studies of 3-alkylamino-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides: a new class of heterocyclic compounds with therapeutical promises

in Tetrahedron (1999), 55

Preparation and pharmacological evaluation of the R- and S-enantiomers of 3-(2-butylamino)-4H- and 3-(3-methyl-2-butylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide, two tissue selective ATP-sensitive potassium channel openers.

in Bioorganic & Medicinal Chemistry (1999), 7(8), 1513-20

The preparation and the pharmacological evaluation of the R- and S-isomers of 3-(2-butylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide (BPDZ 42) and 3-(3-methyl-2-butylamino)-4H-pyrido[4,3-e]-1,2,4 ... [more ▼]

The preparation and the pharmacological evaluation of the R- and S-isomers of 3-(2-butylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide (BPDZ 42) and 3-(3-methyl-2-butylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide (BPDZ 44), two potassium channel openers, is described. Their optical purity was estimated by means of capillary electrophoresis (R- and S-BPDZ 42) and chiral HPLC (R- and S-BPDZ 44). The absolute configuration of each isomer of BPDZ 44 was deduced from crystallographic data. Pharmacological assays performed with the R- and S-isomers of BPDZ 44 revealed only slight differences in their activity on pancreatic B-cells but significant differences in their activity on vascular smooth muscle cells: the R-isomer being sixfold more potent than its corresponding S-isomer. The R-isomer of BPDZ 42 was shown to be more potent than its corresponding S-isomer on the endocrine pancreas. S-BPDZ 44 as well as R- and S-BPDZ 42 were found to exhibit tissue selectivity for the pancreatic versus the vascular smooth muscle tissue. [less ▲]

Recent advances in the chemistry of cholecystokinin receptor ligands (agonists and antagonists)

in Current Medicinal Chemistry (1999), 6

New 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as putative KATP channel openers: design, synthesis and pharmacological evaluation

in Fundamental & Clinical Pharmacology (1999), 13

Enantiomeric Separation of Pirlindole by Liquid Chromatography Using Different Types of Chiral Stationary Phases

in Journal of Pharmaceutical & Biomedical Analysis (1998), 18(4-5), 605-14

The enantioseparation of pirlindole by liquid chromatography (LC) was investigated using three different chiral stationary phases (CSPs) containing either cellulose tris-(3,5-dimethylphenylcarbamate ... [more ▼]

The enantioseparation of pirlindole by liquid chromatography (LC) was investigated using three different chiral stationary phases (CSPs) containing either cellulose tris-(3,5-dimethylphenylcarbamate) (Chiralcel OD-R), ovomucoid (OVM) or beta-cyclodextrin (beta-CD). The effects of the mobile phase pH on retention, enantioselectivity and resolution were studied. Methanol and acetonitrile were tested as organic modifiers while the influence of the addition to the mobile phase of sodium alkanesulfonates or sodium perchlorate was also investigated. Sodium perchlorate was only used on the Chiralcel OD-R column while sodium alkanesulfonates were tested as mobile phase additives on the three kinds of CSPs. The enantioseparation of pirlindole could be obtained on all CSPs tested, the best results with respect to chiral resolution being achieved on the Chiralcel OD-R and the OVM columns. The use of sodium octanesulfonate (NaOS) was found to improve the enantioseparation of pirlindole on the OVM column while enantioselectivity was considerably enhanced by addition of sodium perchlorate on the Chiralcel OD-R column. [less ▲]