Synthesis of some novel N4-(naphtha[1,2-d]thiazol-2-yl)semicarbazides as potential anticonvulsants.

The present invention discloses novel compounds of Formula I: having 11 Beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11Beta-HSD type 1 activity. X-17377

Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1

Synthesis, physicochemical and anticonvulsant properties of new N-phenylamino derivatives of 2-azaspiro[4.4]nonane- and [4.5]decane-1,3-diones: part V.

Design, synthesis, and anticonvulsant activity of new N-Mannich bases derived from spirosuccinimides and spirohydantoins.

Discovery of anticonvulsant activity of abietic acid through application of linear discriminant analysis

Synthesis and anticonvulsant activity of new fluorinated N-phenyl- and N-benzyl-2-azaspiro[4.4]nonane- and [4.5]decane-1,3-dione derivatives: Part III

To continue our systematic SAR studies, two series of N-benzyl- (X = CH2) and N-aminophenyl- (X = NH) derivatives of 2-azaspiro[4.4]nonane (1a–1j) and 2-azaspiro[4.5]decane-1,3-dione (2a–2j) were synthesized, and evaluated in maximum electroshock seizure (MES), subcutaneous pentylenetetrazole (sc.MET) and rotorod (TOX) tests for their anticonvulsant activity. Among those derivatives, the most potent N-aminophenyl-2-azaspiro[4.4]nonane-1,3-dione 1j had ED50 = 76.27 mg kg–1. X-ray structures for two pairs of derivatives with a different linker were solved. Then 3-D data for the active 1j versus less active 2j, both having an imine linker (X = NH), and the respective parent of compounds with a methylene linker (X = CH2) (1a and 2a) were discussed.

Synthesis, physicochemical and anticonvulsant properties of N-benzyl and N-aminophenyl derivatives of 2-azaspiro[4.4]nonane and [4.5]decane-1,3-dione. Part I.

The conversion of enantiomerically enriched (ee >99%) 2α-hydroxypinan-3-one and its oxime (obtained in previously described procedures∗ from α-pinene of 65% ee) into a range of derivatives with potential application in asymmetric synthesis was attempted C2-Symmetrical compounds, ligands for potential catalysts, were synthesized from 2α-hydroxypinan-3-one and either aliphatic or aromatic diamines Reduction or etherification/reduction of selected diiminodiols afforded respective diaminodiols and diaminoethers, which were further transformed into azolium salts Reactions of dipinanediaminoethers with dichlorophenylphosphine and subsequent in situ oxidation of the products afford the respective stable phosphinediamide oxides Four selected compounds were crystallographically studied

Enantiomerically pure α-pinene derivatives from material of 65% enantiomeric purity. Part 2: C2-symmetric N,N'-3-(2α-hydroxy)pinane diimines and diamines

Synthesis, Physicochemical and Anticonvulsant Properties of N‐Benzyl and N‐Aminophenyl Derivatives of 2‐Azaspiro[4.4]nonane and [4.5]Decane‐1,3‐dione. Part 1.

Agnieszka Dzierzawska-Majewska

Papers

Synthesis and anticonvulsant activity of new fluorinated N-phenyl- and N-benzyl-2-azaspiro[4.4]nonane- and [4.5]decane-1,3-dione derivatives: Part III

Synthesis, physicochemical and anticonvulsant properties of N-benzyl and N-aminophenyl derivatives of 2-azaspiro[4.4]nonane and [4.5]decane-1,3-dione. Part I.

Enantiomerically pure α-pinene derivatives from material of 65% enantiomeric purity. Part 2: C2-symmetric N,N'-3-(2α-hydroxy)pinane diimines and diamines

Synthesis, Physicochemical and Anticonvulsant Properties of N‐Benzyl and N‐Aminophenyl Derivatives of 2‐Azaspiro[4.4]nonane and [4.5]Decane‐1,3‐dione. Part 1.