35197-64-9Relevant academic research and scientific papers
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.
Synthesis and characterization of novel phosphonocarboxylate inhibitors of RGGT
Coxon, Fraser,Joachimiak, ?ukasz,Najumudeen, Arafath Kaja,Breen, George,Gmach, Joanna,Oetken-Lindholm, Christina,Way, Rebecca,Dunford, James,Abankwa, Daniel,B?azewska, Katarzyna M.
supporting information, p. 77 - 89 (2014/07/22)
Phosphonocarboxylate (PC) analogs of the anti-osteoporotic drugs, bisphosphonates, represent the first class of selective inhibitors of Rab geranylgeranyl transferase (RabGGTase, RGGT), an enzyme implicated in several diseases including ovarian, breast and skin cancer. Here we present the synthesis and biological characterization of an extended set of this class of compounds, including lipophilic derivatives of the known RGGT inhibitors. From this new panel of PCs, we have identified an inhibitor of RGGT that is of similar potency as the most active published phosphonocarboxylate, but of higher selectivity towards prenyl pyrophosphate synthases. New insights into structural requirements are also presented, showing that only PC analogs of the most potent 3rd generation bisphosphonates inhibit RGGT. In addition, the first phosphonocarboxylate-derived GGPPS weak inhibitor is reported.
MATRIX METALLOPROTEINASE INHIBITORS
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Page/Page column 56-57, (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.
INHIBITORS OF CHECKPOINT KINASES
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Page/Page column 63, (2009/10/09)
The instant invention provides for compounds which comprise substituted thioquinazolinones that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.
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.
Mercaptoacyl matrix metalloproteinase inhibitors: The effect of substitution at the mercaptoacyl moiety
Baxter, Andrew D.,Bhogal, Ranjev,Bird, John B.,Buckley, George M.,Gregory, David S.,Hedger, Paul C.,Manallack, David T.,Massil, Tracy,Minton, Kevin J.,Montana, John G.,Neidle, Stephen,Owen, David A.,Watson, Robert J.
, p. 2765 - 2770 (2007/10/03)
The in vitro potency of orally-active mercaptoacyl matrix metalloproteinase inhibitors is increased by the introduction of appropriate substitutents on the mercaptoacyl moiety.
Synthesis of the Chromophore of Pseudobactin, a Fluorescent Siderophore from Pseudomonas
Kolasa, Teodozyj,Miller, Marvin J.
, p. 4246 - 4255 (2007/10/02)
Protected forms of dihydroxyphenylalanine (DOPA) were converted to the corresponding dihydroquinolin-2-ones 13 by nitration and reductive cyclization.Subsequent N-alkylation with α-halo-γ-aminobutyric acid derivatives provided the carbon framework 12 for the chromophore of pseudobactin.Conversion to protected forms of the fluorescent chromophore 5 was accomplished by reaction of 12 with Lawesson's reagent to produce the corresponding thioamide which was cyclized by reaction with mercuric acetate.
