35197-64-9Relevant articles and documents
Synthesis, biological evaluation and structure-activity relationship of new GABA uptake inhibitors, derivatives of 4-aminobutanamides
Kowalczyk, Paula,Sa?at, Kinga,H?fner, Georg C.,Mucha, Marta,Rapacz, Anna,Podkowa, Adrian,Filipek, Barbara,Wanner, Klaus T.,Kulig, Katarzyna
, p. 256 - 273 (2014/07/08)
Six series of 2-substituted 4-aminobutanamide derivatives were synthesized and evaluated for their ability to inhibit GABA transport proteins mGAT1-4 stably expressed in HEK-293 cell lines. The pIC50 values determined were in the range 4.23-5.23. Two compounds (15b and 15c) were selected for further in vitro studies. These compounds were also subjected to preliminary behavioral studies to evaluate their anticonvulsant, antidepressant-like, and antinociceptive activities in mice. Their influence on motor coordination was also assessed. We report that, among a spectrum of in vivo activities, both 15b and 15c displayed significant activity against pentylenetetrazole (PTZ)-induced seizures.
MATRIX METALLOPROTEINASE INHIBITORS
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, (2012/04/10)
The present invention relates to methyl sulfonamides and N-formamides derivatives of formula (I) and to processes for their syntheses. The invention also relates to pharmacological compositions containing these derivatives and methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatie arthritis, psoriasis, pulmonary fibrosis, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, dry eye, neointimal proliferation which leads to restenosis and ischemic heart failure, stroke, renal disease, tumor metastasis, and other inflammatory disorders characterized by over expression and over activation of an matrix metalloproteinase using the compounds.
THIAZOL-COMPOUNDS AS 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS
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Page/Page column 126; 127-128, (2008/06/13)
The present invention relates to compounds with the formula (I), wherein R1, R2, R3, X, and Y are as defined herein, and also to pharmaceutical compositions comprising the compounds, as well as to the use of the compounds in medicine and for the preparation of a medicament which acts on the human 11-β-hydroxysteroid dehydrogenase type 1 enzyme.