110144-24-6Relevant academic research and scientific papers
Development of potential selective and reversible pyrazoline based MAO-B inhibitors as MAO-B PET tracer precursors and reference substances for the early detection of Alzheimer's disease
Neudorfer, Catharina,Shanab, Karem,Jurik, Andreas,Schreiber, Veronika,Neudorfer, Carolina,Vraka, Chrysoula,Schirmer, Eva,Holzer, Wolfgang,Ecker, Gerhard,Mitterhauser, Markus,Wadsak, Wolfgang,Spreitzer, Helmut
, p. 4490 - 4495 (2014)
Since high MAO-B levels are present in early stages of AD, the MAO-B system can be designated as an appropriate and prospective tracer target of molecular imaging biomarkers for the detection of early AD. According to the preceding investigations of Mishr
Streptonigrin and Lavendamycin Partial Structures. Probes for the Minimum, Potent Pharmacophore of Streptonigrin, Lavendamycin, and Synthetic Quinoline-5,8-diones
Boger, Dale L.,Yasuda, Masami,Mitscher, Lester A.,Drake, Steven D.,Kitos, Paul A.,Thompson, Sandra Collins
, p. 1918 - 1928 (2007/10/02)
The preparation and evaluation of 7-amino-4,8-dioxo-2-(2'-pyridyl)quinoline-6'-carboxylic acid (5a) and 7-amino-2-(2'-aminophenyl)-5,8-dioxoquinoline-5'-carboxylic acid (6a) constituting potential minimum, potent pharmacophores of streptonigrin (1a) and lavendamycin (2a), two structurally related naturally occurring antitumor antibiotics, are detailed.In contrast to observations associated with streptonigrin and lavendamycin in which the C-ring C-6' carboxylic acid potentiates the antitumor, antimicrobial, and cytotoxic properties of the naturally occurring, substituted 7-aminoquinoline-5,8-dione AB ring systems, the C-6'/C-5' carboxylic acid of 5a/6a diminishes the observed antimicrobial and cytotoxic properties of the 2-(2'-pyridyl)- and 2-(2'-aminophenyl)-7-aminoquinoline-5,8-diones.A direct comparison of the antimicrobial and cytotoxic properties of a complete set of stereptonigrin and lavendamycin partial structures is detailed in efforts to define the role peripheral substituents play in potentiating the biological properties of the naturally occurring and synthetic agents bearing the 7-aminoquinoline-5,8-dione AB ring system and in efforts to define the minimum, potent pharmacohore of the naturally occurring antitumor antibiotics.The relationship of these observations to a chemical mechanism of cellular toxicity is discussed.
Synthesis and Characterization of Blocked and Ligand-Appended Hemes Derived from Atropisomeric meso-Diphenylporphyrins
Young, Richard,Chang, C. K.
, p. 898 - 909 (2007/10/02)
The synthesis of a series of sterically blocked and imidazole-appended meso-diphenyletioporphyrins is described.These hybrid porphyrins have good solubility and spectroscopic properties of β-substituted porphyrins as well as the orientation specificity of ortho-position-derivatized tetraphenylporphyrins.The effectiveness of the blocking groups is demonstrated by ferric hemin hydroxide formation in the doubly protected trans-5,15-bis-2,8,12,18-tetraethyl-3,7,13,17-tetramethylporphine, characterized by UV-visible, 1H NMR, and IR spectra and cyclic voltammetry.The advantage of the m-benzyl linkage in enforcing imidazole coordination to ferric hemes is demonstrated by 1H NMR studies on various type of imidazole-appended heme complexes.Several potential binucleating systems have also been prepared by incorporating nonheme chelating ligands to the hybrid porphyrins.
