95460-12-1Relevant academic research and scientific papers
PYRAZOLOPYRIMIDINES AS INHIBITORS OF GLUCOCORTICOID RECEPTOR TRANSLOCATION
-
Paragraph 00863, (2016/08/23)
Provided herein are compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of Glucocorticoid Receptor (GR) translocation. Furthermore, the subject compounds and compositions are useful for the treatment of diseases involved in the hypothalamic-pituitary-adrenal (HPA) axis.
Substituted heterocyclylisoquinolinium salts and compositions and method of use thereof
-
, (2008/06/13)
Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
5,10,15,20-Tetrakis(N-protected-imidazol-2-yl)porphyrins
Milgrom, Lionel R.,Dempsey, Philip J.F.,Yahioglu, Gokhan
, p. 9877 - 9890 (2007/10/03)
It is shown that examples of title porphyrins can be prepared from suitably N-protected imidazole-2-carboxaldehydes and pyrrole in refluxing propionic acid: subsequent deprotection, affords a synthetic route to 5,10,15,20-tetrakis(substituted-imadizol-2-y) porphyrins (TIPs).
Porphyrins with four azole substituents in meso positions: X-ray crystal structure of meso-tetrakis-(1-benzylpyrazol-4-yl)-porphyrin at 200 K
Werner, Andreas,Sanchez-Migallon, Ana,Fruchier, Alain,Elguero, Jose,Fernandez-Castano, Cristina,Foces-Foces, Concepcion
, p. 4779 - 4800 (2007/10/02)
Several new porphyrins have been prepared in improved yields using an established method which was adapted to formylpyrazoles bearing on the pyrazole N1-nitrogen protective groups. The deprotection of N-para-methoxybenzyl and SEM protected meso
Some Benzyl-Substituted Imidazoles, Triazoles, Tetrazoles, Pyridinethiones, and Structural Relatives as Multisubstrate Inhibitors of Dopamine β-Hydroxylase. 4. Structure-Activity Relationships at the Copper Binding Site
Kruse, Lawrence I.,Kaiser, Carl,DeWolf, Walter E.,Finkelstein, Joseph A.,Frazee, James S.,et al.
, p. 781 - 789 (2007/10/02)
Structure-activity relationships (SAR) were determined for novel multisubstrate inhibitors of dopamine β-hydroxylase (DBH; EC 1.14.17.1) by examining the effects upon in vitro inhibitory potencies resulting from structural changes at the copper-binding region of inhibitor.Attempts were made to determine replacement groups for the thione sulfur atom of the prototypical inhibitor 1-(4-hydroxybenzyl)imidazole-2-thione described previously.The synthesis and evaluation of oxygen and nitrogen analogues of the soft thione group demonstrated the sulfur atom to be necessary for optimal activity.An additional series of imidazole-2-thione relatives was prepared in an effort to probe the relationship between the pKa of the ligand group and inhibitor potency.In vitro inhibitory potency was shown not to correlate with ligand pKa over a range of approximately 10 pKa units, and a rationale for this is advanced.Additional ligand modifications were prepared in order to explore bulk tolerance at the enzyme oxygen binding site and to determine the effects of substituting a six-membered ligand group for the five-membered imidazole-2-thione ligand.
